Intermediates for the preparation of phenylsulfonylurea herbicides and plant growth regulators

ABSTRACT

The compounds of the formula (I)    &lt;IMAGE&gt; (I)  in which R1-R4, W, X, Y and Z are as defined in claim 1 are suitable for controlling harmful plants in crops. Their preparation may employ the intermediates of the formulae II and III:    &lt;IMAGE&gt; (II)   &lt;IMAGE&gt; (III)

The invention relates to the technical field of herbicides and plant growth regulators, especially herbicides for the selective control of gramineous and other weeds in crops.

It is known that phenylsulfonylureas which are substituted by heterocycles and carry on the phenyl ring an amino group which may be functionalized possess herbicidal and plant growth-regulating properties (EP-A-1 515, U.S. Pat. Nos. 4,892,946; 4,981,509; EP-A-116 518, U.S. Pat. Nos. 4,664,695 and 4,632,695).

It has now been found that, surprisingly, certain phenylsulfonylureas substituted by heterocycles are particularly highly suitable as herbicides or plant growth regulators.

The present invention relates to compounds of the formula (I) or salts thereof ##STR3## in which R¹ is C₁ -C₆ -alkyl, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, the 3 latter radicals independently of one another being unsubstituted or substituted by one or more radicals from the group comprising halogen, C₁ -C₄ -alkoxy, CONH₂, C₁ -C₄ -alkylthio, CN, CHO, (C₁ -C₆ -alkyl)carbonyl, (C₃ -C₆ -cycloalkyl)carbonyl, C₁ -C₄ -alkylsulfonyl, carboxyl, (C₁ -C₄ -alkoxy)carbonyl, (C₂ -C₄ -alkenyloxy)carbonyl, (C₂ -C₄ -alkynyloxy)carbonyl, NO₂, NH₂, mono- and di-(C₁ -C₆)-alkylamino,

R² is CO--R⁵, COO--R⁶, CO--SR⁷, CO--NR⁸ R⁹, CS--NR¹⁰ R¹¹, CS--OR¹², CS--SR¹³, SO₂ R¹⁴, SO₂ NR¹⁵ R¹⁶,

R³ is COR¹⁷, CO--OR¹⁸, CO--NR¹⁹ R²⁰, CO--SR²¹, CO--O--N═CR²² R²³, CSR²⁴, CSSR²⁵, CS--OR²⁶, CS--NR²⁷ R²⁸, C(═NR²⁹)R³⁰,

R⁴ is H, C₁ -C₆ -alkyl, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, the 3 latter radicals independently of one another being unsubstituted or substituted by one or more halogen radicals,

R⁵ is H, C₁ -C₆ -alkyl, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, the three latter radicals independently of one another being unsubstituted or substituted by one or more radicals from the group comprising halogen, C₁ -C₄ -alkoxy, C₁ -C₄ -alkylthio and NR³¹ R³², or unsubstituted or substituted C₃ -C₈ -cycloalkyl, unsubstituted or substituted phenyl, unsubstituted or substituted heteroaryl or phenyl-C₁ -C₄ -alkyl which is unsubstituted or substituted on the phenyl ring,

R⁶ is C₁ -C₆ -alkyl, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, the three latter radicals independently of one another being unsubstituted or substituted by one or more radicals from the group comprising halogen, C₁ -C₄ -alkoxy, C₁ -C₄ -alkylthio and NR³¹ R³², or C₃ -C₆ -cycloalkyl which is unsubstituted or substituted by one or more radicals from the group comprising halogen, C₁ -C₄ -alkyl and C₁ -C₄ -alkoxy, or C₃ -C₆ -cycloalkyl-C₁ -C₃ -alkyl,

R⁷ is analogous to R⁶

R⁸ is H, C₁ -C₆ -alkyl, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, the 3 latter radicals independently of one another being unsubstituted or substituted by one or more radicals from the group comprising halogen, or (C₁ -C₆ -alkoxy)carbonyl or C₁ -C₄ -alkoxy,

R⁹ is H, C₁ -C₆ -alkyl, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, the 3 latter radicals independently of one another being unsubstituted or substituted by one or more radicals from the group comprising halogen, C₁ -C₄ -alkoxy, C₁ -C₄ -alkylthio and NR³¹ R³², or CO--R³³, CO--OR³⁴, CO--NR³⁵ R³⁶, CS--NR³⁵ R³⁶, CS--R³³ or CS--OR³⁴, or

R⁸, R⁹ taken together are a divalent radical of the formula --(CH₂)₄ --, --(CH₂)₅ --, --CH₂ CH₂ --O--CH₂ CH₂ --, --CH₂ CH₂ NHCH₂ CH₂ --, the 4 latter radicals being unsubstituted or substituted by C₁ -C₄ -alkyl,

R¹⁰ is analogous to R⁸,

R¹¹ is analogous to R⁹,

R¹² is analogous to R⁶,

R¹³ is analogous to R⁶,

R¹⁴ is C₁ -C₆ -alkyl, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, the three latter radicals independently of one another being unsubstituted or substituted by one or more radicals from the group comprising halogen, C₁ -C₄ -alkoxy, C₁ -C₄ -alkylthio and NR³¹ R³²,

R¹⁵ is analogous to R⁸,

R¹⁶ is H, C₁ -C₆ -alkyl, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, the 3 latter radicals independently of one another being unsubstituted or substituted by one or more halogen radicals,

R¹⁷ is analogous to R⁵,

R¹⁸ is C₁ -C₆ -alkyl, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, the three latter radicals independently of one another being unsubstituted or substituted by one or more radicals from the group comprising halogen, C₁ -C₄ -alkoxy, C₁ -C₄ -alkylthio and NR³¹ R³², or C₃ -C₆ -cycloalkyl which is unsubstituted or substituted by one or more radicals from the group comprising halogen, C₁ -C₄ -alkyl and C₁ -C₄ -alkoxy, or C₃ -C₆ -cycloalkyl-C₁ -C₃ -alkyl or H,

R¹⁹ is analogous to R⁸,

R²⁰ is analogous to R⁹,

R²¹ is analogous to R¹⁸,

R²² is H, C₁ -C₄ -alkyl, C₃ -C₅ -alkenyl or C₃ -C₅ -alkynyl,

R²³ is H, C₁ -C₄ -alkyl, C₃ -C₅ -alkenyl or C₃ -C₅ -alkynyl,

R²⁴ is analogous to R¹⁷,

R²⁵ is analogous to R¹⁸,

R²⁶ is analogous to R¹⁸,

R²⁷ is analogous to R⁸,

R²⁸ is analogous to R⁹,

R²⁹ is H, OH, NH₂, NHR³⁷, N(R³⁷)₂, C₁ -C₄ -alkyl, C₁ -C₄ -alkoxy, C₂ -C₄ -alkenyl or C₂ -C₄ -alkynyl, the 4 latter radicals independently of one another being unsubstituted or substituted by one or more radicals from the group comprising halogen, C₁ -C₃ -alkoxy and C₁ -C₃ -alkylthio,

R³⁰ is H, C₁ -C₆ -alkyl, C₁ -C₆ -alkoxy, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, the four latter radicals independently of one another being unsubstituted or substituted by one or more radicals from the group comprising halogen, C₁ -C₃ -alkoxy and C₁ -C₃ -alkylthio,

each R³¹ independently of the others is H, C₁ -C₄ -alkyl, (C₁ -C₄ -alkyl)carbonyl, (C₁ -C₄ -alkoxy)carbonyl or CHO,

each R³² independently of the others is H or C₁ -C₄ -alkyl,

R³³ is analogous to R⁵,

R³⁴ is analogous to R⁶,

R³⁵, R³⁶ independently of one another are H, C₁ -C₆ -alkyl, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, the 3 latter radicals independently of one another being unsubstituted or substituted by one or more halogen radicals,

R³⁷ is C₁ -C₄ -alkyl, C₂ -C₄ -alkenyl or C₂ -C₄ -alkynyl, the three radicals mentioned, independently of one another, being unsubstituted or substituted by one or more radicals from the group comprising halogen, C₁ -C₄ -alkoxy and C₁ -C₄ -alkylthio,

W is O or S,

X and Y independently of one another are hydrogen, halogen, C₁ -C₆ -alkyl, C₁ -C₆ -alkoxy or C₁ -C₆ -alkylthio, the three latter radicals being unsubstituted or substituted by one or more radicals from the group comprising halogen, C₁ -C₄ -alkoxy and C₁ -C₄ -alkylthio, or mono- or di-(C₁ -C₄ -alkyl)amino, C₃ -C₆ -cycloalkyl, C₃ -C₅ -alkenyl, C₃ -C₅ -alkenyloxy or C₃ -C₅ -alkynyloxy, and

Z is CH or N.

In the formula (I) and below, each of the radicals alkyl, alkoxy, haloalkyl, haloalkoxy, alkylamino and alkylthio, and the corresponding unsaturated and/or substituted radicals may be straight-chain or branched in the carbon structure. If not indicated specifically, the carbon structures having from 1 to 4 carbon atoms or, in the case of unsaturated groups, having from 2 to 4 carbon atoms are preferred for these radicals. Examples of alkyl radicals, including those in the composite definitions such as alkoxy, haloalkyl etc., are methyl, ethyl, n- or i-propyl, n-, i-, t- or 2-butyl, pentyls, hexyls such as n-hexyl, i-hexyl and 1,3-dimethylbutyl, heptyls such as n-heptyl, 1-methylhexyl and 1,4-dimethylpentyl; alkenyl and alkynyl radicals have the meaning of the unsaturated radicals corresponding, where possible, to the alkyl radicals, examples of alkenyl are allyl, 1-methylprop-2-en-1-yl, 2-methylprop-2-en-1-yl, but-2-en-1-yl, but-3-en-1-yl, 1-methylbut-3-en-1-yl, 1-methylbut-2-en-1-yl and 1-methylbut-2-en-1-yl; examples of alkynyl are propargyl, but-2 -yn-1-yl, but-3-yn-1-yl and 1-methylbut-3-yn-1-yl.

Halogen is fluorine, chlorine, bromine or iodine. Haloalkyl, haloalkenyl and haloalkynyl are respectively alkyl, alkenyl and alkynyl which are partially or completely substituted by halogen, preferably by fluorine, chlorine and/or bromine and in particular by fluorine or chlorine; examples are CF₃, CHF₂, CH₂ F, CF₃ CF₂, CH₂ FCHCl, CCl₃, CHCl₂, CH₂ CH₂ Cl; examples of haloalkoxy are OCF₃, OCHF₂, OCH₂ F, CF₃ CF₂ O, OCH₂ CF₃ and OCH₂ CH₂ Cl. This applies correspondingly to haloalkenyl and other halo-substituted radicals.

Aryl is a mono-, bi- or polycyclic aromatic system, for example phenyl, naphthyl, tetrahydronaphthyl, indenyl, indanyl, pentalenyl, fluorenyl and the like, preferably phenyl; aryloxy preferably comprises the oxy radicals corresponding to the aryl radicals mentioned, in particular phenoxy. Heteroaryl is a mono-, bi- or polycyclic aromatic system in which at least 1 ring contains one or more heteroatoms, for example pyridyl, pyrimidinyl, pyridazinyl, pyrazinyl, thienyl, thiazolyl, oxazolyl, furyl, pyrrolyl, pyrazolyl and imidazolyl, but also bicyclic or polycyclic aromatic or araliphatic compounds, e.g. quinolinyl, benzoxazolyl etc.

A substituted aryl, heteroaryl, phenyl, benzyl or substituted bicyclic radical containing aromatic structures is, for example, a substituted radical derived from the unsubstituted parent structure, examples of substituents being one or more radicals, preferably 1, 2 or 3 radicals from the group comprising halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, hydroxyl, amino, nitro, cyano, alkoxycarbonyl, alkylcarbonyl, formyl, carbamoyl, mono- and dialkylaminocarbonyl, mono- and dialkylamino, alkylsulfinyl and alkylsulfonyl and, in the case of radicals containing carbon atoms, those having from 1 to 4 carbon atoms, in particular 1 or 2 carbon atoms, being preferred. Preferred substituents in general are those from the group comprising halogen, e.g. fluorine and chlorine, C₁ -C₄ -alkyl, preferably methyl or ethyl, C₁ -C₄ -haloalkyl, preferably trifluoromethyl, C₁ -C₄ -alkoxy, preferably methoxy or ethoxy, C₁ -C₄ -haloalkoxy, nitro and cyano. Particularly preferred substituents are methyl, methoxy and chlorine.

Substituted or unsubstituted phenyl is, for example, phenyl which is unsubstituted or substituted once or more than once, preferably up to three times, by identical or different radicals from the group comprising halogen, C₁ -C₄ -alkyl, C₁ -C₄ -alkoxy, C₁ -C₄ -haloalkyl, C₁ -C₄ -haloalkoxy and nitro, e.g. o-, m- and p-tolyl, dimethylphenyls, 2-, 3- and 4-chlorophenyl, 2,3,4-trifluoro- and -trichlorophenyl, 2,4-, 3,5-, 2,5- and 2,3-dichlorophenyl, o-, m- and p-methoxyphenyl.

A heteroaromatic radical preferably has 5 or 6 members and contains 1, 2 or 3 heteroatoms, preferably from the group comprising N, O and S. The radical may be benzofused. Suitable radicals are those such as oxiranyl, pyrrolidinyl, piperidyl, dioxolanyl, pyrazolyl, morpholyl, furyl, tetrahydrofuryl, indolyl, quinolinyl, pyrimidyl, azepinyl, imidazolyl, triazolyl, thienyl and oxazolyl.

The invention also relates to all the stereoisomers encompassed by formula (I), and mixtures thereof. These compounds of the formula (I) contain one or more asymmetric carbon atoms or double bonds which are not indicated specifically in the formula (I). Formula (I) encompasses all the stereoisomers defined by their specific spatial orientation, such as enantiomers, diastereomers, Z- and E-isomers, all of which can be prepared by conventional methods from mixtures of the stereoisomers or else by stereoselective reactions in combination with the use of stereochemically pure starting substances.

The compounds of the formula (I) may form salts in which the hydrogen of the --SO₂ --NH-- group or else another acidic hydrogen atom (e.g. from COOH etc.) is replaced by a cation which is suitable for agriculture. Examples of these salts are metal salts, in particular alkali metal or alkaline earth metal salts, or else ammonium salts or salts with organic amines. The formation of a salt can also take place by the addition of an acid to basic groups such as amino and alkylamino. Suitable acids in this respect are strong inorganic and organic acids, for example HCl, HBr, H₂ SO₄ or HNO₃.

Primarily for reasons of greater herbicidal activity, improved selectivity and/or increased ease of preparation, compounds of the formula (I) or salts thereof of particular interest are those in which

R¹ is C_(1-C) ₄ -alkyl, C₂ -C₄ -alkenyl or C₂ -C₄ -alkynyl, preferably C₁ -C₄ -alkyl, allyl or propargyl, or

R² is CO--R⁵, COOR⁶, CO--NR⁸ R⁹, CS--NR¹⁰ R¹¹, SO₂ R¹⁴ or SO₂ NR¹⁵ R¹⁶, or

R³ is COR¹⁷, COOR¹⁸, CONR¹⁹ R²⁰ or CO--ON═CR²² R²³, preferably COOR¹⁸, or

R⁴ is H or C₁ -C₄ -alkyl, preferaby H or methyl, or

R⁵ is H, C₁ -C₆ -alkyl which is unsubstituted or substituted by one or more radicals from the group comprising halogen, or by C₁ -C₄ -alkoxy, C₁ -C₄ -alkylthio or NR³¹ R³², or C₃ -C₆ -cycloalkyl, unsubstituted or substituted phenyl, unsubstituted or substituted benzyl or unsubstituted or substituted heteroaryl, preferably H, C₁ -C₆ -alkyl, C₁ -C₄ -haloalkyl, cyclopropyl, cyclopentyl, cyclohexyl, phenyl or heteroaryl, the two latter radicals being unsubstituted or substituted by one or more radicals from the group comprising C₁ -C₄ -alkyl, C₁ -C₄ -alkoxy and halogen, or

R⁶ is C₁ -C₆ -alkyl, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, C₁ -C₆ -haloalkyl or C₃ -C₆ -cycloalkyl, preferably C₁ -C₄ -alkyl, C₁ -C₄ -haloalkyl, allyl, propargyl or C₃ -C₆ -cycloalkyl, or

R⁷ is C₁ -C₄ -alkyl,

R⁸ is hydrogen, C₁ -C₆ -alkyl, C₁ -C₄ -haloalkyl. C₁ -C₄ -alkoxy or (C₁ -C₄ -alkoxy)carbonyl,

R⁹ is hydrogen, C₁ -C₆ -alkyl which is unsubstituted or substituted by one or more radicals from the group comprising halogen, C₁ -C₄ -alkoxy and NR³¹ R³², or CO--R³³, CO--OR³⁴ or CO--NR³⁵ R³⁶, or

R⁸ and R⁹ taken together are a divalent radical of the formula --(CH₂)₄ --, --(CH₂)₅ -- or --CH₂ CH₂ --O--CH₂ CH₂ --, or

R¹⁴ is C₁ -C₆ -alkyl or C₁ -C₆ -haloalkyl, preferably C₁ -C₄ -alkyl or C₁ -C₄ -haloalkyl, or

R¹⁵, R¹⁶ independently of one another are hydrogen or C₁ -C₄ -alkyl, or

R¹⁷ is hydrogen or C₁ -C₄ -alkyl, C₁ -C₄ -haloalkyl, C₃ -C₆ -cycloalkyl, phenyl or heteroaryl, the two latter radicals being unsubstituted or substituted, or

R¹⁸ is hydrogen, C₁ -C₄ -alkyl, C₂ -C₆ -alkenyl or C₂ -C₆ -alkynyl, the 3 latter radicals being unsubstituted or substituted by one or more radicals from the group comprising halogen, C₁ -C₄ -alkoxy, C₁ -C₄ -alkylthio and NR³¹ R³², or C₃ -C₆ -cycloalkyl or C₃ -C₆ -cycloalkyl-C₁ -C₃ -alkyl, or

R²² is hydrogen or C₁ -C₂ -alkyl, or

R²³ is hydrogen or C₁ -C₂ -alkyl, or

R²⁹ is hydrogen, hydroxyl, amino, NHCH₃, N(CH₃)₂, C₁ -C₄ -alkyl or C₁ -C₄ -alkoxy,

R³⁰ is hydrogen or C₁ -C₄ -alkyl, or

each R³¹ independently of the others is H or C₁ -C₄ -alkyl, or

each R³² independently of the others is H or C₁ -C₄ -alkyl, or

R³³ is hydrogen, C₁ -C₄ -alkyl, C₁ -C₄ -haloalkyl, C₃ -C₆ -cycloalkyl or phenyl which is unsubstituted or substituted by one or more radicals from the group comprising halogen, C₁ -C₄ -alkyl and C₁ -C₄ -alkoxy, or

R³⁴ is C₁ -C₄ -alkyl, allyl, propargyl or cycloalkyl, or

R³⁵ is hydrogen or C₁ -C₄ -alkyl, or

R³⁶ is hydrogen or C₁ -C₄ -alkyl, or

X is C₁ -C₄ -alkyl, C₁ -C₄ -alkoxy, C₁ -C₄ -haloalkyl, C₁ -C₄ -alkylthio, halogen or mono- or di-(C₁ -C₂ -alkyl)amino, preferably methyl, ethyl, methoxy, ethoxy, methylthio, ethylthio, chlorine, NHCH₃ or N(CH₃)₂, or

Y is C₁ -C₄ -alkyl, C₁ -C₄ -alkoxy, C₁ -C₄ -haloalkyl or C₁ -C₄ -alkylthio, preferably methyl, ethyl, methoxy or ethoxy,

or preferably those compounds of the formula (I) or salts thereof in which two or more of the particular or preferred definitions mentioned above for the radicals R¹ to R³⁶ in formula (I) are present in combination.

Preferred compounds of the formula (I) or salts thereof are those in which

R¹ is methyl, ethyl, n-propyl, i-propyl or allyl,

R² is CO--R⁵, COOR⁶, CO--NR⁸ R⁹, CS--NR¹⁰ R¹¹, SO₂ R¹⁴ or SO₂ NR¹⁵ R¹⁶,

R⁵ is H, C₁ -C₄ -alkyl, C₁ -C₂ -haloalkyl, cyclopropyl, phenyl, benzyl or heteroaryl having 5 or 6 ring atoms, the 3 latter radicals being unsubstituted or substituted by one or more halogen atoms,

R⁶ is C₁ -C₄ -alkyl, allyl, propargyl or cyclopropyl,

R⁸ is H, C₁ -C₄ -alkyl, C₁ -C₄ -haloalkyl or (C₁ -C₄ -alkoxy)carbonyl,

R⁹ is H or C₁ -C₄ -alkyl,

R¹⁰ is H or C₁ -C₄ -alkyl,

R¹¹ is H or C₁ -C₄ -alkyl,

R¹⁴ is C₁ -C₄ -alkyl,

R¹⁵ is H or C₁ -C₄ -alkyl and

R¹⁶ is H or C₁ -C₄ -alkyl.

R⁵ is particularly preferably H, CH₃, C₂ H₅, n- or i-C₃ H₇, n-, i-, t- or 2-butyl, n-pentyl, CF₃, CH₂ Cl, CHCl₂, CCl₃, CH₂ Br, CH₂ CCl₃, cyclopropyl, phenyl, thienyl, furyl or pyridyl, in which case the 4 latter radicals may be substituted by from 1 to 3 halogen atoms.

The present invention also relates to processes for the preparation of the compounds of the formula (I) according to the invention or salts thereof, which comprises

a) reacting a compound of the formula (II) ##STR4## with a heterocyclic carbamate of the formula (III) ##STR5## in which R* is unsubstituted or substituted phenyl or C₁ -C₄ -alkyl, or

b) reacting a sulfonyl isocyanate of the formula (IV) ##STR6## with an amino heterocycle of the formula (V) ##STR7## or c) reacting a compound of the formula (II) with a (thio)isocyanate of the formula (X) ##STR8## in the presence of a base, the radicals R¹ to R⁴, W, X, Y and Z in the above formulae (II) to (V) and (X) being as defined in formula (I) and, in the case of variants a) and b), the compounds initially obtained being those of the formula (I) in which W=O.

The reaction of the compounds of the formulae (II) and (III) is preferably carried out base-catalyzed in an inert organic solvent, for example dichloromethane, acetonitrile, dioxane or THF, at temperatures between 0° C., preferably 20° C., and the boiling point of the solvent. Examples of the base used are organic amine bases, such as 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU), especially when R*=(substituted) phenyl (cf. EP-A-44 807), or trimethylaluminum or triethylaluminum, the latter especially when R*=alkyl (cf. EP-A-166 516).

The sulfonamides (II) and the sulfonyl isocyanates (IV) are new compounds. They and their preparation are also subjects of the invention.

The compounds of the formula (II) are obtained, for example, starting from compounds of the formula (VI) ##STR9## in which R¹, R² and R³ are as defined in formula (I), by reaction with a strong acid (cf. in this respect WO 89/10921).

Examples of suitable strong acids are mineral acids, such as H₂ SO₄ or HCl, or strong organic acids such as trifluoroacetic acid. The elimination of the tert-butyl protective group is carried out, for example, at temperatures from -20° C. to the respective reflux temperature of the reaction mixture, preferably at 0° C. The reaction can be carried out without solvent or else in an inert solvent, for example dichloromethane or trichloromethane.

The compounds of the formula (VI) are obtained, for example, from the compounds of the formula (VI')-which corresponds to the formula (VI) but in which R² =H-by reaction with suitable electrophiles such as acid chlorides, acid anhydrides, isocyanates, thioisocyanates, sulfonyl chlorides or amidosulfonyl chlorides (cf. in this respect: A. L. J. Beckniter in J. Zabicky, "The Chemistry of Amides", pp. 73-185, Interscience, New York, 1970, E. J. Corey et al., Tetrahedron Lett. 1978, 1051; H. J. Saunders, R. J. Slocombe, Chem. Rev. 43, 203 (1948); S. Ozaki, Chem. Rev. 72, 457, 469 (1972); G. zolB, Arzneim.-Forsch. 33, 2 (1983); Houben-Weyl-Hagemann, "Methoden der organischen Chemie [Methods of Organic Chemistry]", 4th edition, vol. E4, p. 485 ff., Thieme verlag Stuttgart, 1983; J. Golinsky, M. Mahosza, Synthesis 1978, 823; Houben-Weyl-Muller, "Methoden der organischen Ghemie", 4th edition, vol. IX, pp. 338-400 and 605-622, Thieme Verlag Stuttgart, 1955; Houben-Weyl-Klarmann, "Methoden der organischen Chemie", 4th edition, vol. E 11/2, pp. 1020-22, Thieme Verlag Stuttgart, 1985; S. Krishnamurthey, Tetrahedron Lett. 23, 3315 (1982)).

The N-monosubstituted aminobenzene derivatives, for example N-alkylaminobenzene derivatives, which are required for this purpose, of the formula (VI') (see formula (VI), R² =H) are obtained by monoalkylation of the anilines of the formula (VI") (=formula (VI), R¹ =H and R² =H) by standard methods. For example, the N-acylation of the anilines of the formula (VI") with carboxylic acid chlorides or carboxylic acid anhydrides gives the corresponding N-acyl-anilines. The subsequent reduction of the acylamino group to the analogous N-monosubstituted amino group, e.g. alkylamino group (see above) using suitable reducing agents, for example borane/dimethyl sulfide complex, gives the aniline derivatives of the formula (VI') (=formula (VI), R² =H) in very good yields; see S. Krishnamurthey, Tetrahedron Leet. 23, 3315 (1982).

The aniline derivatives mentioned of the formula (VI') (=formula (VI), R¹ and R² =H) are obtained by methods known from the literature, by reduction of the nitro group in compounds (VII), for example by hydrogenation with hydrogen in the presence of a suitable catalyst, as Pd/C or Raney nickel, or by reduction with iron in a medium acidified with acetic acid. (cf. in this respect: H. Berrie, G. T. Neuhold, F. S. Spring, J. Chem, Soc. 1952, 2042; M. Freifelder, "Catalytic Hydrogenation in Organic Synthesis: Procedures and Commentary", J. Wiley and Sons, New York (1978) chapter 5).

The aromatic sulfonamides of the formula (VII) can be obtained from the sulfonic acids of the formula (VIII). ##STR10##

The sulfonic acid group in compounds (VIII) is first converted to the sulfonyl chlorides, for example by standard methods such as the reaction of phosphorus oxychloride or thionyl chloride with potassium salts of the corresponding sulfonic acids in inert solvents such as acetonitrile and/or sulfolane, or without solvent, by heating at reflux (cf. Houben-Weyl-Klamann, "Methoden der organischen Chemie", 4th edition, vol. E XI/2, pp. 1067-1073, Thieme Verlag Stuttgart, 1985).

The formation of sulfonamide from the sulfonyl chlorides using tert-butylamine in ethanol gives the compounds (VII) in good yields (cf. analogous reactions in WO 89/10921).

The sulfonic acids of the formula (VIII) can be prepared from 2-methyl-5-nitrobenzenesulfonic acid, which is available commercially.

The substituent R³ is introduced by oxidation of the methyl group of 2-methyl-5-nitrobenzenesulfonic acid using standard methods, such as the reaction with potassium permanganate to give the carboxyl group, followed if desired by derivatization, for example esterification or amidation (cf. in this respect: Houben-Weyl-Falbe: "Methoden der organischen Chemie", 4th edition, vol. E V/1, Thieme Verlag Stuttgart, 1985, pp. 199-202).

A wide variation in the radical R³ can be obtained using a range of standard reactions:

Carboxylic acid amides are obtainable by reacting acid anhydrides or acid chlorides with amines (cf. in this respect: A. L. J. Beckwith in J. Zabicky, "The Chemistry of Amides", pp. 73-185, Interscience, New York 1970).

Thiocarboxylic acid S-esters can be prepared from carboxylic acids and thiols with carbonyl activation, for example using diphenylphosphinyl chloride (cf. in this respect: D. Scholz, D. Eigner, Monatsh. Chemie 110, 759 (1979), S. Yamada et al., J. Org. Chem. 39, 3302 (1974)).

Thiocarboxylic acid O-esters can be prepared by reacting carboxylic acid esters with suitable reagents, for example P₄ S₁₀ (cf. in this respect: S. O. Lauresson et al., Bull. Soc. Chim. Belg. 87, 293 (1978); T. Nishiwak et al., Chem. Lett. 1980, 401).

Thiocarboxylic acid amides are obtained from carboxylic acid amides by "sulfurization", for example with phosphorus pentasulfide (Houben-Weyl-Falbe, "Methoden der organischen Chemie", 4th edition, vol. E 5/2, pp. 1242-1247 (and literature cited therein), Thieme Verlag Stuttgart, 1985).

Aldehydes can be synthesized from carboxylic acids or esters using a range of reducing agents (Houben-Weyl-Falbe, "Methoden der organischen Chemie", 4th edition, vol. E 3, p. 418 ff., Thieme Verlag Stuttgart, 1983).

Functionalized aldehyde derivatives, for example oximes, oxime ethers, hydrazones etc., can be obtained from the aldehydes by condensation with the corresponding amines (cf. in this respect: Houben-Weyl-Muller, "Methoden der organischen Chemie", 4th edition, vol. 7/1, pp. 453-474, Thieme Verlag Stuttgart, 1954).

N-Alkoxy-carboxylic acid imide esters can be prepared from hydroxamic acid bromide derivatives and alcoholates (E. C. Tayler, F. Kienzle, J. Org. Chem. 36, 233 (1971).

Carboxylic acid imide esters can be obtained from carboxylic acid chloride imides and corresponding alcoholates (cf. in this respect: H. Bohme, O. Muller, Chem. Ber. 98, 1450 (1965); G. Bock, Chem. Ber. 100, 2870 (1967).

O-Acyl oximes can be prepared, for example, by reacting carboxylic acid anhydrides with ketoximes (cf. in this respect: S. Bittner, Y. Knobler, M. Frankel, Tetrahedron Lett. 1965, 95).

Hydroxamic acid amides can be obtained by reacting hydroxamic acid chloride derivatives with amines (cf. in this respect: Houben-Weyl-Muller, "Methoden der organischen Chemie", 4th edition, vol. 10/4, p. 209 ff., Thieme Verlag Stuttgart, 1968).

Alternatively, the sulfonamides of the formula (II) in which R¹ and R² are not H can be obtained by aminolysis of the corresponding sulfonyl chlorides of the formula (IXb) ##STR11## which in turn are readily obtainable from the sulfonic acids (IXa) by the standard methods mentioned (see abovementioned reactions of (VIII) to (VII)).

The compounds (IXa) can in turn be obtained from the nitrobenzenesulfonic acid (VIII) by the sequence of reactions

(1) reduction by analogy with reduction of (VII),

(2) N-alkylation and

(3) N-acylation,

the latter being as described in the preparation of (VI).

The carbamates of the formula (III) which are required for the reaction of compounds (II) by variant a) are known from the literature or can be prepared by analogy with known processes (cf. EP-A-70 804 or U.S. Pat. No. 4,480,101).

The compounds of the formulae (IV) and (V) which can be employed for the process variants b) can also be prepared from the abovementioned compounds of the formulae (III) and (VIII) and their precursors by, or by analogy with, methods which are known in general terms.

The phenylsulfonyl isocyanates of the formula (IV) can be prepared for example, by analogy with the processes from EP-A-184 385 starting from compounds of the formula (II) and using, for example, phosgene.

The reaction of the compounds (IV) with the amino heterocycles of the formula (V) is preferably carried out in inert aprotic solvents, for example dioxane, acetonitrile or tetrahydrofuran, at temperatures between 0° C. and the boiling temperature of the solvent.

The (thio) isocyanates of the formula (X) can be prepared by methods known from the literature (cf. EP-A-232 067, EP-A-166 516).

The reaction of compounds of the formula (X) with sulfonamides of the formula (II) is carried out at temperatures of between -10° C. and +10° C., preferably between +20° and +80° C., in an inert aprotic solvent, for example acetone or acetonitrile, in the presence of a suitable base such as triethylamine or potassium carbonate.

The salts of the compounds of the formula (I) are preferably prepared in inert solvents such as water, methanol, acetone, dichloromethane, tetrahydrofuran, toluene or heptane, at temperatures from 0° to 100° C. Examples of bases suitable for the preparation of the salts according to the invention are alkali metal carbonates, such as potassium carbonate, alkali metal and alkaline earth metal hydroxides, ammonia or a suitable amine base, such as triethylamine or ethanolamine. Examples of acids suitable for salt formation are HCl, HBr, H₂ SO₄ or HNO₃.

The inert solvents referred to in the abovementioned process variants are in each case solvents which are inert under the respective reaction conditions, but which are not necessarily inert under any reaction conditions.

The compounds of the formula (I) according to the invention or their salts have an excellent herbicidal activity against a broad range of economically important monocotyledon and dicotyledon harmful plants. The active substances also act efficiently on perennial weeds which produce shoots from rhizomes, root stocks or other perennial organs and which are difficult to control. In this context, it does not matter whether the substances are applied before sowing, pre-emergence or post-emergence. Specifically, examples may be mentioned of some representatives of the monocotyledon and dicotyledon weed flora which can be controlled by the compounds according to the invention, without the mention intending restriction to certain species.

Examples of weed species on which the active substance acts efficiently are, from amongst the monocotyledons, Avena, Lolium, Alopecurus, Phalaris, Echinochloa, Digitaria, Setaria and also Cyperus species from the annual sector and from amongst the perennial species Agropyron, Cynodon, Imperata and Sorghum, and also perennial Cyperus species.

In the case of the dicotyledon weed species, the range of action extends to species such as, for example, Galium, Viola, Veronica, Lamium, Stellaria, Amaranthus, Sinapis, Ipomoea, Matricaria, Abutilon and Sida from amongst the annuals, and Convolvulus, Cirsium, Rumex and Artemisia in the case of the perennial weeds.

The active substances according to the invention likewise effect outstanding control of weeds which occur under the specific conditions of rice-growing, such as, for example, Sagittaria, Alisma, Eleocharis, Scirpus and Cyperus.

If the compounds according to the invention are applied to the soil surface before germination, then the weed seedlings are either prevented completely from emerging, or the weeds grow until they have reached the cotyledon stage but then their growth stops and, eventually, after three to four weeks have elapsed, they die completely.

If the active substances are applied post-emergence on the green parts of the plants, growth likewise stops drastically a very short time after the treatment and the weed plants remain at the growth stage of the point in time of application, or they die completely after a certain time, so that in this manner competition by the weeds, which is harmful to the crop plants, is eliminated at a very early point in time and in a sustained manner.

Even though the compounds according to the invention have an excellent herbicidal activity against monocotyledon and dicotyledon weeds, crop plants of economically important crops, such as, for example, wheat, barley, rye, rice, maize, sugar beet, cotton and soya, are damaged not at all, or only to a negligible extent. For these reasons, the present compounds are highly suitable for selectively controlling unwanted plant growth in agricultural crop plants.

In addition, the substances according to the invention exhibit outstanding growth-regulatory properties in crop plants. They intervene to regulate the plant metabolism and can therefore be employed so as to have a specific influence on substances contained in plants, and for facilitating harvesting, for example by initiating desiccation and growth compression. Furthermore, they are also suitable for the general control and inhibition of unwanted vegetative growth, without killing off the plants in the process. Inhibition of vegetative growth plays an important role in many monocotyledon and dicotyledon crops, since it can reduce or completely prevent lodging.

The compounds according to the invention can be used in the form of wettable powders, emulsifiable concentrates, sprayable solutions, dusting agents or granules in the conventional formulations. The invention therefore also relates to herbicidal and plant growth-regulating agents comprising compounds of the formula (I) or salts thereof.

The compounds of the formula (I) or salts thereof can be formulated in a variety of ways, as predetermined by the biological and/or chemicophysical parameters. The following possibilities are therefore suitable for formulation: wettable powders (WP), water-soluble powders (SP), water-soluble concentrates, emulsifiable concentrates (EC), emulsions (EW) such as oil-in-water and water-in-oil emulsions, sprayable solutions, suspension concentrates (SC), dispersions on an oil or water base, oil-miscible solutions, capsule suspensions (CS), dusting agents (DP) seed-dressing agents, granules for scattering and soil application, granules (GR) in the form of microgranules, sprayable granules, coated granules and adsorption granules, water-dispersible granules (WG), water-soluble granules (SG), ULV formulations, microcapsules and waxes.

These individual formulation types are known in principle and are described, for example in: Winnacker-Kuchler, "Chemische Technologie [Chemical Technology]", Volume 7, C. Hauser Verlag Munich, 4th Ed., 1986; Wade van Valkenburg, "Pesticide Formulations", Mercel Dekker N.Y., 1973; K. Martens, "Spray Drying" Handbook, 3rd Ed. 1979, G. Goodwin Ltd. London.

The formulation auxiliaries required, such as inert materials, surfactants, solvents and other additives, are likewise known and are described, for example, in: Watkins, "Handbook of Insecticide Dust Diluent and Carriers", 2nd Ed., Darland Books, Caldwell N.J., H. v. Olphen, "Introduction to Clay Colloid Chemistry", 2nd Ed., J. Wiley & Sons, N.Y.; C. Marsden, "Solvents Guide", 2nd Ed., Interscience, N.Y. 1963; McCutcheon's "Detergents and Emulsifiers Annual", MC Publ. Corp. Ridgewood N.J.; Sisley and Wood, "Encyclopedia of Surface Active Agents", Chem. Publ. Co. Inc., N.Y. 1964; Schonfeldt, "Grenzflachenaktive Athylenoxidaddukte" [Surface-active Ethylene Oxide Adducts] Wiss. Verlagsgesell., Stuttgart 1976; Winnacker-Kuchler, "Chemische Technologie [Chemical Technology]", Volume 7, C. Hauser Verlag Munich, 4th Ed. 1986.

Combinations with other pesticidally active substances, such as insecticides, acaricides, herbicides, fungicides, safeners, fertilizers and/or growth regulators may also be prepared on the basis of these formulations, for example in the form of a ready-to-use formulation or as a tank mix.

Wettable powders are preparations which are uniformly dispersible in water and which, besides the active substance, also contain surfactants of ionic and/or nonionic type (wetting agents, dispersants), for example polyethoxylated alkylphenols, polyethoxylated fatty alcohols, polyethoxylated fatty amines, fatty alcohol polyglycol ether sulfates, alkanesulfonates, alkylbenzenesulfonates, sodium ligninsulfonate, sodium 2,2'-dinaphthylmethane-6,6'-disulfonate, sodium dibutylnaphthalenesulfonate, or alternatively sodium oleoylmethyltaurinate, in addition to a diluent or inert substance. The wettable powders are prepared by finely grinding the herbicidal active substances, for example, in conventional apparatus such as hammer mills, blower mills and air-jet mills, and mixing them simultaneously or subsequently with the formulation auxiliaries.

Emulsifiable concentrates are prepared by dissolving the active substance in an organic solvent, for example butanol, cyclohexanone, dimethylformamide, xylene and also higher-boiling aromatic compounds or hydrocarbons or mixtures of the organic solvents, with the addition of one or more surfactants of ionic and/or nonionic type (emulsifiers). Examples of emulsifiers which can be used are: calcium salts of an alkylarylsulfonic acid such as Ca dodecylbenzenesulfonate, or nonionic emulsifiers, such as fatty acid polyglycol esters, alkylaryl polyglycol ethers, fatty alcohol polyglycol ethers, propylene oxide/ethylene oxide condensation products, alkyl polyethers, sorbitan esters, such as sorbitan fatty acid esters or polyoxyethylene sorbitan esters, such as polyoxyethylene sorbitan fatty esters.

Dusting agents are obtained by grinding the active substance with finely divided solid substances, for example talc or natural clays, such as kaolin, bentonite, pyrophyllite or diatomaceous earth.

Suspension concentrates may be based on water or oil. They can be prepared by, for example, wet grinding using conventional bead mills with the possible addition of surfactants as already mentioned, for example, above for the other types of formulation.

Emulsions, for example oil-in-water emulsions (EW), can be prepared, for example, by means of stirrers, colloid mills and/or static mixers, using aqueous organic solvents and, if desired, surfactants, for example as already listed above for the other types of formulation.

Granules can be produced either by spraying the active substance onto adsorptive, granulated inert material or by applying active substance concentrates onto the surface of carriers, such as sand, kaolinites or granulated inert material, by means of binders, for example polyvinyl alcohol, sodium polyacrylate or, alternatively, mineral oils. Suitable active substances can also be granulated in the manner which is conventional for the production of fertilizer granules, if desired in a mixture with fertilizers.

Water-dispersible granules are generally prepared by conventional methods such as spray-drying, fluidized-bed granulation, plate granulation, mixing using high-speed mixers and extrusion without solid inert material.

The agrochemical formulations generally contain from 0.1 to 99% by weight and in particular from 0.1 to 95% by weight of active substance of the formula (I) or salts thereof.

The concentration of active substance in wettable powders is, for example, about 10 to 90% by weight; the remainder to 100% by weight is composed of conventional formulation components. In the case of emulsifiable concentrates, the concentration of active substance can be about 1 to 90, preferably 5 to 80% by weight. Formulations in the form of dusts usually contain 1 to 30, preferably 5 to 20% by weight of active substance, sprayable solutions about 0.05 to 80, preferably 2 to 50% by weight. In the case of water-dispersible granules, the active substance content depends partly on whether the active compound is liquid or solid and on which granulation auxiliaries, fillers etc. are used. In the case of the water-dispersible granules, the content of active substance is, for example, between 1 and 95% by weight and preferably between 10 and 80% by weight.

In addition, the active substance formulations mentioned contain, if appropriate, the adhesives, wetting agents, dispersants, emulsifiers, penetrants, preservatives, frost protectors and solvents, fillers, carriers and colorants, antifoams, evaporation inhibitors and agents influencing the pH and the visocity which are conventional in each case.

Combination partners which can be employed for the active substances according to the invention in mixed formulations or as a tank mix are, for example, known active substances as described in, for example, Weed Research 26, 441-445 (1986), or "The Pesticide Manual", 9th edition, The British Crop Protection Council, 1990/91, Bracknell, England, and the literature quoted therein. Examples of herbicides known from the literature which can be combined with the compounds of the formula (I) are the following active substances (note: the compounds are either given by their common name in accordance with the International Organization for Standardization (ISO) or by the chemical name, together if appropriate with a common code number): acetochlor; acifluorfen; aclonifen; AKH 7088, i.e. [[[1-[5-[2-chloro-4-(trifluoromethyl)phenoxy]-2-nitrophenyl]-2-methoxyethylidene]amino]oxy]acetic acid and its methyl ester; alachlor; alloxydim; ametryn; amidosulfuron; amitrol; AMS, i.e. ammonium sulfamate; anilofos; asulam; atrazin; aziprotryn; barban; BAS 516 H, i.e. 5-fluoro-2-phenyl-4H-3,1-benzoxazin-4-one; benazolin; benfluralin; benfuresate; bensulfuron-methyl; bensulide; bentazone; benzofenap; benzofluor; benzoylprop-ethyl; benzthiazuron; bialaphos; bifenox; bromacil; bromobutide; bromofenoxim; bromoxynil; bromuron; buminafos; busoxinone; butachlor; butamifos; butenachlor; buthidazole; butralin; butylate; carbetamide; CDAA, i.e. 2-chloro-N,N-di-2-propenylacetamide; CDEC, i.e. 2-chloroallyl diethyldithiocarbamate; CGA 184927, i.e. 2-[4-[(5-chloro-3-fluoro-2-pyridinyl)oxy]phenoxy]propanoic acid and its 2-propynyl ester; chlomethoxyfen; chloramben; chlorazifop-butyl; pirifenop-butyl; chlorbromuron; chlorbufam; chlorfenac; chlorflurecol-methyl; chloridazon; chlorimuron ethyl; chlornitrofen; chlorotoluron; chloroxuron; chlorpropham; chlorsulfuron; chlorthaldimethyl; chlorthiamid; cinmethylin; cinosulfuron; clethodim; clomazone; clomeprop; cloproxydim; clopyralid; cyanazine; cycloate; cycloxydim; cycluron; cyperquat; cyprazine; cyprazole; 2,4-DB; dalapon; desmediphan; desmetryn; di-allate; dicamba; dichlobenil; dichlorprop; diclofop-methyl; diethatyl; difenoxuron; difenzoquat; diflufenican; dimefuron; dimethachlor; dimethametryn; dimethazone; clomazon; dimethipin; dimetrasulfuron, cinosulfuron; dinitramine; dinoseb; dinoterb; diphenamid; dipropetryn; diquat; dithiopyr; diuron; DNOC; eglinazine-ethyl; EL 177, i.e. 5-cyano-1-(1,1-dimethylethyl)-N-methyl-3H-pyrazole-4-carboxamide; endothal; EPTC; esprocarb; ethafluralin; ethametsulfuron-methyl; ethidimuron; ethiozin; ethofumesate; F5231, i.e. N-[2-chloro-4-fluoro-5-[4-(3-fluoropropyl)-4,5-dihydro-5-oxo-1H-tetrazol-1-yl]phenyl]ethanesulfonamide; F6285, i.e. 1-[5-(N-methylsulfonyl)amino-2,4-dichlorophenyl]-3-methyl-4-difluoromethyl-1,2,4-triazol-5-one; fenoprop; fenoxan, s. clomazon; fenoxaprop-ethyl; fenuron; flamprop-methyl; flazasulfuron; fluazifop and its ester derivatives; fluchloralin; flumetsulam; N-[2,6-difluorophenyl]-5-methyl-1,2,4-triazolo[1,5a]pyrimidin-2-sulfonamide; flumeturon; flumipropyn; fluorodifen; fluoroglycofen-ethyl; fluridone; flurochloridone; fluroxypyr; flurtamone; fomesafen; fosamine; furyloxyfen; glufosinate; glyphosate; halosaten; haloxyfop and its ester derivatives; hexazinone; Hw 52, i.e. N-(2,3-dichlorophenyl)-4-(ethoxymethoxy)benzamide; imazamethabenzmethyl; imazapyr; imazaquin; imazethamethapyr; imazethapyr; imazosulfuron; ioxynil; isocarbamid; isopropalin; isoproturon; isouron; isoxaben; isoxapyrifop; karbutilate; lactofen; lenacil; linuron; MCPA; MCPB; mecoprop; mefenacet; mefluidid; metamitron; metazachlor; methabenzthiazuron; metham; methazole; methoxyphenone; methyldymron; metobromuron; metolachlor; metoxuron; metribuzin; metsulfuron-methyl; MH; molinate; monalide; monocarbamide dihydrogensulfate; monolinuron; monuron; MT 128, i.e. 6 -chloro-N-(3-chloro-2-propenyl)-5-methyl-N-phenyl-3-pyridazinamine; MT 5950, i.e. N-[3-chloro-4-(1-methylethyl)phenyl]-2-methylpentanamide; naproanilide; napropamide; naptalam; NC 310, i.e. 4-(2,4-dichlorobenzoyl)-1-methyl-5-benzyloxypyrazole; neburon; nicosulfuron; nipyraclophen; nitralin; nitrofen; nitrofluorfen; norflurazon; orbencarb; oryzalin; oxadiazon; oxyfluorfen; paraquat; pebulate; pendimethalin; perfluidone; phenisopham; phenmedipham; picloram; piperophos; piributicarb; pirifenop-butyl; pretilachlor; primisulfuron-methyl; procyazine; prodiamine; profluralin; proglinazine-ethyl; prometon; prometryn; propachlor; propanil; propaquizafop and its ester derivatives; propazine; propham; propyzamide; prosulfalin; prosulfocarb; prynachlor; pyrazolinate; pyrazon; pyrazosulfuron-ethyl; pyrazoxyfen; pyridate; quinclorac; quinmerac; quinofop and its ester derivatives, quizalofop and its ester derivatives; quizalofopethyl; quizalofop-p-tefuryl; renriduron; dymron; S 275, i.e. 2-[4-chloro-2-fluoro-5-(2-propynyloxy)phenyl]-4,5,6,7-tetrahydro-2H-indazole; S 482, i.e. 2-[7-fluoro-3,4-dihydro-3-oxo-4-(2-propynyl)-2H-1,4-benzoxazin-6-yl]-4,5,6,7-tetrahydro-1H-isoindole-1,3(3H)-dione; secbumeton; sethoxydim; siduron; simazine; simetryn; SN 106279, i.e. 2-[[7-[2-chloro-4-(trifluoromethyl)phenoxy]-2-naphthyl]oxy]propanoic acid and its methyl ester; sulfometuron-methyl; sulfazuron; flazasulfuron; TCA; tebutam; tebuthiuron; terbacil; terbucarb; terbuchlor; terbumeton; terbuthylazine; terbutryn; TFH 450, i.e. N,N-diethyl-3-[(2-ethyl-6-methylphenyl)sulfonyl]-1H-1,2,4-triazole-1-carboxamide; thiazafluoron; thifensulfuron-methyl; thiobencarb; tiocarbazil; tralkoxydim; tri-allate; triasulfuron; triazofenamide; tribenuronmethyl; triclopyr; tridiphane; trietazine; trifluralin; trimeturon; vernolate; WL 110547, i.e. 5-phenoxy-1-[3-(trifluoromethyl)phenyl]-1 H-tetrazole.

For use, the formulations, present in commercially available form, are diluted, if appropriate, in a customary manner, for example using water in the case of wettable powders, emulsifiable concentrates, dispersions and water-dispersible granules and then applied to plants, plant parts or agriculturally or industrially utilized soil, on which the plants are located, or in which they grow or are present as seed. Preparations in the form of dusts or granules for soil application and scattering, and also sprayable solutions, are usually not further diluted with other inert substances before use.

The application rate required for the compounds of the formula I varies with the external conditions, such as, inter alia, temperature, humidity, and the nature of the herbicide used. It can vary within wide limits, for example between 0.001 and 10.0 kg/ha or more of active substance; preferably, however, it is between 0.005 and 5 kg/ha.

A) Chemical Examples

a) 2-Carboxy-nitrobenzenesulfonic acid 400.0 g (2.53 mol) of potassium permanganate are added in portions at 80° C. over a period of 2 h to a solution of 106.0 g (0.40 mol) of 2-methyl-5-nitrobenzenesulfonic acid and 80.0 g (0.58 mol) of potassium carbonate in 1300 ml of water. The reaction temperature is maintained at between 80° and 95° C. After stirring for a further 4 h, the solid formed is filtered off. The filtrate is acidified with concentrated hydrochloric acid (pH=1). The colorless 2-carboxy-5-nitrobenzenesulfonic acid which has precipitated is filtered off with suction through a Buchner funnel and dried at about 50° C./100 torr (82.0 g; 83.7% of theory). Melting point: >300° C.

b) 2-Methoxycarboxy-5-nitrobenzenesulfonic acid

A suspension of 190.0 g (0.77 mol) of 2-carboxy-5-nitrobenzenesulfonic acid, 10 ml of DMF and 250 ml (3.43 mol) of thionyl chloride is heated at boiling for 3 h. After separating off the insoluble constituents by filtration, the filtrate is concentrated. 200 ml (4.94 mol) of methanol are added to the residue which results. When addition is complete the reaction mixture is cooled to 0° C. The solid which precipitates is filtered off and dried. 70.9 g (35.3% of theory) of colorless, crystalline 2-methoxycarbonyl-5-nitrobenzenesulfonic acid (m.p.: 92°-94° C.) are thus obtained. By distilling off the volatile components from the mother liquor, a second fraction (62.5 g, 31.1% of theory) is obtained.

c) 2-Methoxycarbonyl-5-nitrobenzenesulfonyl chloride

A solution of 17.3 g (0.27 mol) of potassium hydroxide (88% strength) and 100 ml of methanol is added carefully with vigorous stirring to a solution of 70.9 g (0.27 mol) of 2-methoxycarbonyl-5-nitrobenzenesulfonic acid in 300 ml of methanol. The mixture is cooled to 0° C. and the salt which is precipitated is filtered off, dried and then suspended in 150 ml of sulfolane, 150 ml of acetonitrile and 10 ml of dimethylformamide. After the dropwise addition of 100 ml (1.07 mol) of phosphorus oxychloride, the mixture is heated at boiling for 2.5 h. The reaction mixture is then poured into ice-water. The 2-methoxycarbonyl-5-nitrobenzenesulfonyl chloride (60.1 g, 70% of theory) which has precipitated is filtered off with suction through a Buchner funnel and freed from traces of solvent under reduced pressure. Melting point: 86°-88° C.

d) N-tert-Butyl-2-methoxycarbonyl-5-nitrobenzenesulfonamide

50 ml (0.48 mol) of tert-butylamine are slowly added dropwise at 0° C. to a solution of 34.4 g (0.12 mol) of 2-methoxycarbonyl-5-nitrobenzenesulfonyl chloride in 200 ml of ethyl acetate and 250 ml of ethanol. The reaction solution is then stirred for a further 10 min at room temperature. After the addition of 500 ml of water, a colorless solid crystallizes out. It is filtered off and dried to give 28.1 g (89% of theory) of N-tert-butyl-2-methoxycarbonyl-5-nitrobenzenesulfonyl chloride. m.p.: 121°-124° C.

e) N-tert-Butyl-5-amino-2-methoxycarbonylbenzenesulfonamide

25.08 g (0.079 mol) of N-tert-butyl-2-methoxycarbonyl-5-nitrobenzenesulfonamide are dissolved in 1000 ml of MeOH. 0.50 g of Pd-C (10%) is added and the mixture is shaken under a hydrogen atmosphere (1 atm) until the uptake of hydrogen has finished. The catalyst is separated off and the solvent is removed by distillation. The residue is induced to crystallize by stirring with a little ethyl acetate. The resulting N-tert-butyl-5-amino-2-methoxycarbonylbenzenesulfonamide (18.3 g; 80.9% of theory) melts at 193° C.

f) N-tert-Butyl-5-formylamino-2-methoxycarbonylbenzenesulfonamide

6.5 ml of formic acid are carefully added at 0° C. to 13 ml of acetic anhydride. The mixture is subsequently heated at 50°-60° C. for 2 h. A solution of 16.0 g (0.056 mol) of N-tert-butyl-5-amino-2-methoxycarbonylbenzenesulfonamide in 50 ml of DMF is then added dropwise at 0° C. The cooling bath is removed and the mixture is stirred for a further 4 h at room temperature. The reaction mixture is then taken up in 800 ml of ethyl acetate and washed with three times 150 ml of water. The organic phase is dried over magnesium sulfate, the solvent is distilled off, and the residue is recrystallized from ethyl acetate/n-heptane. The product is N-tert-butyl-5-formylamino-2-methoxycarbonylbenzenesulfonamide (14.23 g, 82% of theory) which melts at 113°-114° C.

g) N-tert-Butyl-2-methoxycarbonyl-5-methylaminobenzenesulfonamide

9.92 g (0.032 mol) of N-tert-butyl-5-formylamino-2-methoxycarbonylbenzenesulfonamide are dissolved in 50 ml of CHCl₃, and then 5 ml (0.053 mol) of boranedimethyl sulfide complex are added at 0° C. After 1 h at 0° C. and 3 h at room temperature the reaction mixture is cooled to 0° C. 30 ml of methanol are added and the mixture is washed with water. The organic phase is dried over magnesium sulfate, the solvent is removed by distillation, and 9.23 g (98% of theory) of N-tert-butyl-2-methoxycarbonyl-5-methylaminobenzenesulfonamide are obtained. m.p.: 120°-124° C.

h) N-tert-Butyl-5-[N-(ethoxycarbonylaminothiocarbonyl)methylamino]-2-methoxycarbonylbenzenesulfonamide

1.20 g (4.0 mmol) of N-tert-butyl-2-methoxycarbonyl-5-methylaminobenzenesulfonamide is dissolved in 5 ml of anhydrous DMF, and 0.60 g (4.3 mmol) of 95% strength ethoxycarbonyl isothiocyanate is added. After 3 h at room temperature the mixture is taken up in ethyl acetate and washed with 1N hydrochloric acid and water. The organic phase is dried over magnesium sulfate and the solvent is removed by distillation. The residue is taken up in a little ethyl acetate and precipitated with heptane at -25° C. The precipitate is filtered off with suction and dried to give 1.29 g (75% of theory) of colorless N-tert-butyl-5-[N-(ethoxycarbonylaminothiocarbonyl)methylamino]-2-methoxycarbonylbenzenesulfonamide. m.p.: 110° C.

i) 5-[N-(Ethoxycarbonylaminothiocarbonyl)methylamino]-2-methoxycarbonylbenzenesulfonamide

1.05 g (2.4 mmol) of N-tert-butyl-5-[N-(ethoxycarbonylaminothiocarbonyl)methylamino]-2-methoxycarbonylbenzenesulfonamide is stirred for 18 h in 15 ml of trifluoroacetic acid at room temperature. Volatile components are then removed by distillation at 12 torr/50° C. The residue is suspended in toluene. The suspension is again concentrated at 12 torr/50° C. to give a highly viscous residue (0.85 g, 93% of theory) which is reacted directly without further purification to give the corresponding sulfonylurea (cf. Example j).

j) N-[(4,6-Dimethoxypyrimidin-2-yl)aminocarbonyl]-5-[N-(ethoxycarbonylaminothiocarbonyl)methylamino]-2-methoxycarbonylbenzenesulfonamide (see tabular Example 2192)

1.2 ml of DBU is added to a suspension of 0.69 g (1.84 mmol) of 5-[N-(ethoxycarbonylaminothiocarbonyl)methylamino]-2-methoxycarbonylbenzenesulfonamide and 0.55 g (1.99 mmol) of 4,6-dimethoxy-2-phenoxycarbonylaminopyrimidine in 5 ml of acetonitrile. The mixture is stirred for 17 h at room temperature and the solvent is then removed by distillation. The residue is taken up in water and washed with diethyl ether. The aqueous phase is acidified with concentrated hydrochloric acid (pH=1) and produces a colorless precipitate, which is filtered off and induced to crystallize by stirring with a little methanol. The resulting product is 0.61 g (60% of theory) of N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-5-[N-(ethoxycarbonylaminothiocarbonyl)methylamino]-2-methoxycarbonylbenzenesulfonamide. m.p.: 144°-145° C.

k) 5-[N-(Acetylmethylamino)-N-(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-2-methoxycarbonylbenzenesulfonamide (see Table 1, Example 89)

0.45 ml of DBU is added to a mixture of 0.75 g (2.6 mmol) of 5-(N-acetylmethylamino)-2-methoxycarbonylbenzenesulfonamide and 0.73 g (2.6 mmol) of 4,6-dimethoxy-2-(phenoxycarbonylamino)pyrimidine in 10 ml of CH₃ CN. The mixture is worked up in analogy to Example j) to give 0.59 g of the desired sulfonylurea, m.p.: 197° C.

l) 2-Methoxycarbonyl-5-(N-methoxycarbonyl-N-methylamino)benzenesulfonyl isocyanate

5.0 g of 2-methoxycarbonyl-5-(N-methoxycarbonyl-N-methylamino)benzenesulfonamide are suspended in 17 ml of 1,2-dichloroethane. 4 ml of thionyl chloride are added and the reaction mixture is heated at boiling for 5 h. The reaction mixture is cooled to room temperature, 0.3 ml of pyridine is added, phosgene is passed into the reaction mixture, and the solution is heated at reflux for 4 h. The reaction mixture is concentrated to give 6.3 g of an oil which is employed directly in the subsequent reaction (Examples m, n, o).

m) 2-Methoxycarbonyl-5-(N-methoxycarbonyl-N-methylamino)-N-[(4,6-dimethylpyrimidin-2-yl)aminocarbonyl]benzenesulfonamide (see Table 1, Example 1,183)

A solution of 2.1 g of 2-methoxycarbonyl-5-(N-methoxycarbonylmethylamino)benzenesulfonyl isocyanate (Example 1)) in 20 ml of dichloroethane is added to a solution of 0.8 g of 2-amino-4,6-dimethylpyrimidine in 20 ml of dichloroethane. The reaction mixture is stirred for 8 h at 40° C. and then concentrated. The residue is induced to form the product by stirring intensively and successively with 1N hydrochloric acid and methanol, to give 0.47 g of the desired sulfonylurea as a solid foam:

¹ H NMR (DMSO, 80 MHz): δ (ppm)=2.5 (s, 6H, 2 CH₃), 3.3 (s, 3H, N--CH₃), 3.7 (s, 3H, O--CH₃), 3.9 (s, 3H, OCH₃), 7.0 (s, 1H, H_(pyrimidine)), 7.8 (s, 2H, 3-H and 4H), 8.1 (s, 1H, 6-H), 10.6 (s, 1H, NH), 13.3 (s, 1H, SO₂ -NH).

n) N-[(4-Chloro-6-methoxypyrimidin-2-yl)aminocarbonyl]-2-methoxycarbonyl-5-(N-methoxycarbonyl-N-methylamino)benzenesulfonamide (see Table 1, Example 1,185)

By analogy with Example m), 0.9 g of 2-amino-4-chloro-6-methoxypyrimidine is reacted with 2.1 g of 2-methoxycarbonyl-5-(N-methoxycarbonyl-N-methylamino)benzenesulfonyl isocyanate (Example 1)). Yield: 0.45 g of the desired sulfonylurea as a solid foam:

¹ H NMR (DMSO, 80 MHz): δ (ppm)=3.3 (s, 3H, N-CH₃), 3.7 (s, 3H, O--CH₃), 3.8 (s, 3H, O--CH₃), 4.0 (s, 3H, O--CH₃), 6.8 (s, 1H, H_(pyrimidine)), 7.7 (s, 2H, 3-H and 4-H), 10.9 (s, 1H, NH), 12.0 (s, 1H, SO₂ -NH).

o) N-[N-(4-Methoxy-6-methyltriazin-2-yl)aminocarbonyl]-2-methoxcarbonyl-5-(N-methoxycarbonyl-N-methylamino)benzenesulfonamide (see Table 1, Example 1,180)

By analogy with Example m), 0.85 g of 2-amino-4-methoxy-6-methyltriazine is reacted with 2.1 g of 2-methoxycarbonyl-5-(N-methoxycarbonyl-N-methylamino)benzenesulfonyl isocyanate (Example 1)). Yield: 0.47 g of the desired sulfonylurea as a solid foam:

¹ H NMR (DMSO, 80 MHz): δ (ppm)=2.4 (s, 3H, CH₃), 3.3 (s, 3H, N--CH₃), 3.7 (s, 3H, OCH₃), 3.8 (s, 3H, OCH₃), 4.0 (s, 3H, O--CH₃), 7.8 (s, 2H, 3-H, 4-H), 8.1 (s, 1H, 6-H), 11.0 (s, 1H, NH), 12.3 (s, 14, SO₂ NH).

The remainder of the compounds described in Table 1 are obtained in a manner analogous to Examples a) to o).

The following abbreviations are used in Table 1:

No.=Example number

m.p.=solidification point (melting point) in °C

Me=methyl

Et=ethyl

Pr=n-propyl

n-Pr=n-propyl

i-Pr=i-propyl

c-Pr=cyclopropyl

Bu=butyl

Ph=phenyl.

                                      TABLE 1                                      __________________________________________________________________________      ##STR12##                                                                     No.                                                                               R.sup.1                                                                           R.sup.2    R.sup.3                                                                               R.sup.4                                                                           X   Y     Z  m.p.                                   __________________________________________________________________________      1 Me COCH.sub.2 OMe                                                                            CO.sub.2 Me                                                                           H  OMe OMe   CH                                         2 Et "          "      "  "   "     "                                          3 Me COCH.sub.2 NHCO.sub.2                                                                     "      "  "   "     "                                               Me                                                                        4 Me COCH.sub.2 SMe                                                                            "      "  "   "     "                                          5 "  "          "      Me "   "     "                                          6 "  "          "      H  OMe Me    N                                          7 "  "          "      "  Me  Me    CH                                         8 Et "          "      "  "   "     "                                          9 "  "          "      "  OMe "     N                                          10                                                                               "  "          "      "  OMe OMe   N                                          11                                                                               Me CHO        "      "  OMe OMe   CH 177-182                                 12                                                                               "  "          "      "  OMe OMe   N                                          13                                                                               "  "          "      "  OMe Me    N                                          14                                                                               "  "          "      "  OMe Me    CH                                         15                                                                               "  "          "      "  NMe.sub.2                                                                          OCH.sub.2 CF.sub.3                                                                   N                                          16                                                                               "  "          "      "  Me  Me    CH                                         17                                                                               "  "          "      "  Me  Me    N                                          18                                                                               "  "          "      "  Cl  OMe   CH                                         19                                                                               "  "          "      Me OMe OMe   CH                                         20                                                                               "  "          "      Me OMe Me    N                                          21                                                                               "  "          CO.sub.2 Et                                                                           H  OMe OMe   CH                                         22                                                                               "  "          "      "  OMe Cl    CH                                         23                                                                               "  "          "      "  Me  Me    CH                                         24                                                                               "  "          "      "  OMe Me    N                                          25                                                                               "  "          "      "  NMe.sub.2                                                                          OCH.sub.2 CF.sub.3                                                                   N                                          26                                                                               "  "          "      Me OMe OMe   CH                                         27                                                                               "  "          "      Me OMe Me    N                                          28                                                                               "  "          CO.sub.2 -n-Pr                                                                        H  OMe OMe   CH                                         29                                                                               "  "          "      "  OMe OMe   N                                          30                                                                               "  "          "      "  OMe Me    N                                          31                                                                               "  "          "      "  Me  Me    CH                                         32                                                                               "  "          "      "  OMe Cl    CH                                         33                                                                               "  "          "      Me Me  OMe   N                                          34                                                                               "  "          "      Me OMe OMe   CH                                         35                                                                               Me CHO        CO.sub.2 -i-Pr                                                                        H  OMe OMe   CH                                         36                                                                               "  "          "      "  OMe OMe   N                                          37                                                                               "  "          "      "  OMe Me    N                                          38                                                                               "  "          "      "  OMe Cl    CH                                         39                                                                               "  "          "      "  Me  Me    CH                                         40                                                                               "  "          "      "  SMe NEt.sub.2                                                                            N                                          41                                                                               "  "          CO.sub.2 -i-Pr                                                                        Me OMe Me    N                                          42                                                                               "  "          "      Me OMe OMe   CH                                         43                                                                               Me CHO        CO.sub.2 -Allyl                                                                       H  OMe OMe   CH                                         44                                                                               Et CHO        CO.sub.2 Me                                                                           H  OMe OMe   CH                                         45                                                                               "  "          "      "  OMe Me    N                                          46                                                                               "  "          "      "  Me  Me    CH                                         47                                                                               "  "          "      "  Cl  OMe   CH                                         48                                                                               "  "          "      Me OMe OMe   CH                                         49                                                                               "  "          "      Me OMe Me    N                                          50                                                                               "  "          CO.sub.2 Et                                                                           H  OMe OMe   CH                                         51                                                                               "  "          "      "  OMe Me    CH                                         52                                                                               "  "          "      "  Cl  OMe   CH                                         53                                                                               "  "          "      "  OMe Me    N                                          54                                                                               "  "          "      Me OMe OMe   CH                                         55                                                                               "  "          "      Me OMe Me    N                                          56                                                                               "  "          CO.sub.2 -n-Pr                                                                        H  OMe OMe   CH                                         57                                                                               "  "          "      "  OMe Me    N                                          58                                                                               "  "          "      "  OMe Cl    CH                                         59                                                                               "  "          "      "  Me  Me    CH                                         60                                                                               "  "          "      Me OMe OMe   CH                                         61                                                                               "  "          "      Me OMe Me    N                                          62                                                                               "  "          CO.sub.2 -i-Pr                                                                        H  OMe OMe   CH                                         63                                                                               "  "          "      "  OMe Me    N                                          64                                                                               "  "          "      "  Me  Me    CH                                         65                                                                               "  "          "      Me OMe Me    N                                          66                                                                               n-Pr                                                                              CHO        CO.sub.2 Me                                                                           H  OMe OMe   CH                                         67                                                                               "  "          "      "  OMe Cl    CH                                         68                                                                               "  "          "      "  Me  Me    CH                                         69                                                                               "  "          "      "  OMe Me    N                                          70                                                                               "  "          "      Me OMe OMe   CH                                         71                                                                               "  "          "      Me OMe Me    N                                          72                                                                               n-Pr                                                                              "          CO.sub.2 Et                                                                           H  OMe Me    N                                          73                                                                               "  "          "      "  OMe OMe   CH                                         74                                                                               "  "          "      "  Me  Me    CH                                         75                                                                               "  "          CO.sub.2 n-Pr                                                                         "  OMe OMe   CH                                         76                                                                               i-Pr                                                                              "          CO.sub.2 Me                                                                           H  OMe OMe   CH                                         77                                                                               "  "          "      "  OMe Me    N                                          78                                                                               "  "          "      "  Me  Me    CH                                         79                                                                               "  "          "      "  Cl  OMe   N                                          80                                                                               "  "          "      Me OMe Me    N                                          81                                                                               "  "          "      Me OMe OMe   CH                                         82                                                                               Allyl                                                                             "          CO.sub.2 Me                                                                           H  OMe OMe   CH                                         83                                                                               "  "          "      "  OMe Cl    CH                                         84                                                                               "  "          "      "  Me  Me    CH                                         85                                                                               "  "          "      "  OMe Me    N                                          86                                                                               "  "          CO.sub.2 Et                                                                           "  OMe OMe   CH                                         87                                                                               "  "          CO.sub.2 n-Pr                                                                         "  OMe OMe   CH                                         88                                                                               "  "          CO.sub.2 i-Pr                                                                         "  OMe OMe   CH                                         89                                                                               Me COCH.sub.3 CO.sub.2 Me                                                                           "  OMe OMe   CH 197° C.                          90                                                                               "  "          "      "  OMe OMe   N                                          91                                                                               "  "          "      "  OMe Me    N                                          92                                                                               "  "          "      "  OMe Me    CH                                         93                                                                               "  "          "      "  NMe.sub.2                                                                          OCH.sub.2 CF.sub.3                                                                   N                                          94                                                                               "  "          "      "  Me  Me    CH                                         95                                                                               "  "          "      "  Me  Me    N                                          96                                                                               "  "          "      "  Cl  OMe   CH                                         97                                                                               "  "          "      Me OMe OMe   CH                                         98                                                                               "  "          "      Me OMe Me    N                                          99                                                                               "  "          CO.sub.2 Et                                                                           H  OMe OMe   CH                                        100                                                                               "  "          "      "  OMe Cl    CH                                        101                                                                               "  "          "      "  Me  Me    CH                                        102                                                                               "  "          "      "  OMe Me    N                                         103                                                                               "  "          "      "  NMe.sub.2                                                                          OCH.sub.2 CF.sub.3                                                                   N                                         104                                                                               "  "          "      Me OMe OMe   CH                                        105                                                                               "  "          "      Me OMe Me    N                                         106                                                                               "  "          CO.sub.2 -n-Pr                                                                        H  OMe OMe   CH                                        107                                                                               "  "          "      "  OMe OMe   N  "                                      108                                                                               "  "          "      "  OMe Me    N                                         109                                                                               "  "          "      "  Me  Me    CH                                        110                                                                               "  "          "      "  OMe Cl    CH                                        111                                                                               "  "          "      Me Me  OMe   N                                         112                                                                               "  "          "      Me OMe OMe   CH                                        113                                                                               Me COCH.sub.3 CO.sub.2 -i-Pr                                                                        H  OMe OMe   CH                                        114                                                                               "  "          "      "  OMe OMe   N                                         115                                                                               "  "          "      "  OMe Me    N                                         116                                                                               "  "          "      "  OMe Cl    CH                                        117                                                                               "  "          "      "  Me  Me    CH                                        118                                                                               "  "          "      "  SMe NEt.sub.2                                                                            N                                         119                                                                               "  "          CO.sub.2 -i-Pr                                                                        Me OMe Me    N                                         120                                                                               "  "          "      Me OMe OMe   CH                                        121                                                                               Me COCH.sub.3 CO.sub.2 -Allyl                                                                       H  OMe OMe   CH                                        122                                                                               Et "          CO.sub.2 Me                                                                           H  OMe OMe   CH                                        123                                                                               "  "          "      "  OMe Me    N                                         124                                                                               "  "          "      "  Me  Me    CH                                        125                                                                               "  "          "      "  Cl  OMe   CH                                        126                                                                               "  "          "      Me OMe OMe   CH                                        127                                                                               "  "          "      Me OMe Me    N                                         128                                                                               "  "          CO.sub.2 Et                                                                           H  OMe OMe   CH                                        129                                                                               "  "          "      "  OMe Me    CH                                        130                                                                               "  "          "      "  Cl  OMe   CH                                        131                                                                               "  "          "      "  OMe Me    N                                         132                                                                               "  "          "      Me OMe OMe   CH                                        133                                                                               "  "          "      Me OMe Me    N                                         134                                                                               "  "          CO.sub.2 -n-Pr                                                                        H  OMe OMe   CH                                        135                                                                               "  "          "      "  OMe Me    N                                         136                                                                               "  "          "      "  OMe Cl    CH                                        137                                                                               "  "          "      "  Me  Me    CH                                        138                                                                               "  "          "      Me OMe OMe   CH                                        139                                                                               "  "          "      Me OMe Me    N                                         140                                                                               "  "          CO.sub.2 -i-Pr                                                                        H  OMe OMe   CH                                        141                                                                               "  "          "      "  OMe Me    N                                         142                                                                               "  "          "      "  Me  Me    CH                                        143                                                                               "  "          "      Me OMe Me    N                                         144                                                                               n-Pr                                                                              COCH.sub.3 CO.sub.2 Me                                                                           H  OMe OMe   CH 160° C.                         145                                                                               "  "          "      "  OMe Cl    CH                                        146                                                                               "  "          "      "  Me  Me    CH                                        147                                                                               "  "          "      "  OMe Me    N                                         148                                                                               "  "          "      Me OMe OMe   CH                                        149                                                                               "  "          "      Me OMe Me    N                                         150                                                                               n-Pr                                                                              "          CO.sub.2 Et                                                                           H  OMe Me    N                                         151                                                                               "  "          "      "  OMe OMe   CH                                        152                                                                               "  "          "      "  Me  Me    CH                                        153                                                                               "  "          CO.sub.2 -n-Pr                                                                        "  OMe OMe   CH                                        154                                                                               i-Pr                                                                              "          CO.sub.2 Me                                                                           H  OMe OMe   CH                                        155                                                                               "  "          "      "  OMe Me    N                                         156                                                                               "  "          "      "  Me  Me    CH                                        157                                                                               "  "          "      "  Cl  OMe   N                                         158                                                                               "  "          "      Me OMe Me    N                                         159                                                                               "  "          "      Me OMe OMe   CH                                        160                                                                               Allyl                                                                             "          CO.sub.2 Me                                                                           H  OMe OMe   CH                                        161                                                                               "  "          "      "  OMe Cl    CH                                        162                                                                               "  "          "      "  Me  Me    CH                                        163                                                                               "  "          "      "  OMe Me    N                                         164                                                                               "  "          CO.sub.2 Et                                                                           H  OMe OMe   CH                                        165                                                                               "  "          CO.sub.2 -n-Pr                                                                        "  OMe OMe   CH                                        166                                                                               "  "          CO.sub.2 -i-Pr                                                                        "  OMe OMe   CH                                        167                                                                               Me COCH.sub.2 CH.sub.3                                                                       CO.sub.2 Me                                                                           H  OMe OMe   CH                                        168                                                                               "  "          "      "  OMe OMe   N                                         169                                                                               "  "          "      "  SMe Me    N                                         170                                                                               "  "          "      "  OMe Me    N                                         171                                                                               "  "          "      "  OMe Me    CH                                        172                                                                               "  "          "      "  NMe.sub.2                                                                          OCH.sub.2 CF.sub.3                                                                   N                                         173                                                                               "  "          "      "  Me  Me    CH                                        174                                                                               "  "          "      "  Me  Me    N                                         175                                                                               "  "          "      "  Cl  OMe   CH                                        176                                                                               "  "          "      Me OMe OMe   CH                                        177                                                                               "  "          CO.sub.2 Me                                                                           Me OMe Me    N                                         178                                                                               "  "          CO.sub.2 Et                                                                           H  OMe OMe   CH                                        179                                                                               "  "          "      "  OMe Cl    CH                                        180                                                                               "  "          "      "  Me  Me    CH                                        181                                                                               "  "          "      "  OMe Me    N                                         182                                                                               "  "          "      "  NMe.sub.2                                                                          OCH.sub.2 CF.sub.3                                                                   N                                         183                                                                               "  "          "      Me OMe OMe   CH                                        184                                                                               "  "          "      Me OMe Me    N                                         185                                                                               "  "          CO.sub.2 -n-Pr                                                                        H  OMe OMe   CH                                        186                                                                               "  "          "      "  OMe OMe   N                                         187                                                                               "  "          "      "  OMe Me    N                                         188                                                                               "  "          "      "  Me  Me    CH                                        189                                                                               "  "          "      "  OMe Cl    CH                                        190                                                                               "  "          "      Me Me  OMe   N                                         191                                                                               "  "          "      "  OMe OMe   CH                                        192                                                                               Me COCH.sub.2 CH.sub.3                                                                       CO.sub.2 -i-Pr                                                                        H  OMe OMe   CH                                        201                                                                               Et "          CO.sub.2 -Me                                                                          H  OMe OMe   CH                                        202                                                                               "  "          "      "  OMe Me    N                                         203                                                                               "  "          "      "  Me  Me    CH                                        204                                                                               "  "          "      "  Cl  OMe   CH                                        205                                                                               "  "          "      Me OMe OMe   CH                                        206                                                                               "  "          "      "  OMe Me    N                                         207                                                                               "  "          CO.sub.2 Et                                                                           H  OMe OMe   CH                                        193                                                                               "  "          "      "  OMe OMe   N                                         194                                                                               "  "          "      "  OMe Me    N                                         195                                                                               "  "          "      "  OMe Cl    CH                                        196                                                                               "  "          "      "  Me  Me    CH                                        197                                                                               "  "          "      "  SMe NEt.sub.2                                                                            N                                         198                                                                               "  "          "      Me OMe Me    N                                         199                                                                               "  "          "      "  OMe OMe   CH                                        200                                                                               Me COCH.sub.2 CH.sub.3                                                                       CO.sub.2 -Allyl                                                                       H  OMe OMe   CH                                        208                                                                               "  "          "      "  OMe Me    CH                                        209                                                                               "  "          "      "  Cl  OMe   CH                                        210                                                                               "  "          "      "  OMe Me    N                                         211                                                                               "  "          "      Me OMe OMe   CH                                        212                                                                               "  "          "      "  "   Me    N                                         213                                                                               "  "          CO.sub.2 -n-Pr                                                                        H  OMe OMe   CH                                        214                                                                               "  "          "      "  OMe Me    N                                         215                                                                               "  "          "      "  OMe Cl    CH                                        216                                                                               "  "          "      "  Me  Me    CH                                        217                                                                               "  "          "      Me OMe OMe   CH                                        218                                                                               "  "          "      "  OMe Me    N                                         219                                                                               "  "          CO.sub.2 -i-Pr                                                                        H  OMe OMe   CH                                        220                                                                               "  "          "      "  OMe Me    N                                         221                                                                               "  "          "      "  Me  Me    CH                                        222                                                                               "  "          "      Me OMe Me    N                                         223                                                                               n-Pr                                                                              COCH.sub.2 CH.sub.3                                                                       CO.sub.2 Me                                                                           H  OMe OMe   CH                                        224                                                                               "  "          "      "  OMe Cl    CH                                        225                                                                               "  "          "      "  Me  Me    CH                                        226                                                                               "  "          "      "  OMe Me    N                                         227                                                                               "  "          "      Me OMe OMe   CH                                        228                                                                               "  "          "      Me OMe Me    N                                         229                                                                               n-Pr                                                                              "          CO.sub.2 Et                                                                           H  OMe Me    N                                         230                                                                               "  "          "      "  OMe OMe   CH                                        231                                                                               "  "          "      "  Me  Me    CH                                        232                                                                               "  "          CO.sub.2 -n-Pr                                                                        "  OMe OMe   CH                                        233                                                                               i-Pr                                                                              "          CO.sub.2 Me                                                                           H  OMe OMe   CH                                        234                                                                               "  "          "      "  OMe Me    N                                         235                                                                               "  "          "      "  Me  Me    CH                                        236                                                                               "  "          "      "  Cl  OMe   N                                         237                                                                               "  "          "      Me OMe Me    N                                         238                                                                               "  "          "      Me OMe OMe   CH                                        239                                                                               Allyl                                                                             "          CO.sub.2 Me                                                                           H  OMe OMe   CH                                        240                                                                               "  "          "      "  OMe Cl    CH                                        241                                                                               "  "          "      "  Me  Me    CH                                        242                                                                               "  "          "      "  OMe Me    N                                         243                                                                               "  "          CO.sub.2 Et                                                                           H  OMe OMe   CH                                        244                                                                               "  "          CO.sub.2 -n-Pr                                                                        "  OMe OMe   CH                                        245                                                                               "  "          CO.sub.2 -i-Pr                                                                        "  OMe OMe   CH                                        246                                                                               Me CO-n-Pr    CO.sub.2 Me                                                                           H  OMe OMe   CH                                        247                                                                               "  "          "      "  OMe OMe   N                                         248                                                                               "  "          "      "  OMe Me    N                                         249                                                                               "  "          "      "  OMe Me    CH                                        250                                                                               "  "          "      "  NMe.sub.2                                                                          OCH.sub.2 CF.sub.3                                                                   N                                         251                                                                               "  "          "      "  Me  Me    CH                                        252                                                                               "  "          "      "  Me  Me    N                                         253                                                                               "  "          "      "  Cl  OMe   CH                                        254                                                                               "  "          "      Me OMe OMe   CH                                        255                                                                               "  "          "      Me OMe Me    N                                         256                                                                               "  "          CO.sub.2 Et                                                                           H  OMe OMe   CH                                        257                                                                               "  "          "      "  OMe Cl    CH                                        258                                                                               "  "          "      "  Me  Me    CH                                        259                                                                               "  "          "      "  OMe Me    N                                         260                                                                               "  "          "      "  NMe.sub.2                                                                          OCH.sub.2 CF.sub.3                                                                   N                                         261                                                                               "  "          "      Me OMe OMe   CH                                        262                                                                               "  "          "      Me OMe Me    N                                         263                                                                               "  "          CO.sub.2 -n-Pr                                                                        H  OMe OMe   N                                         264                                                                               "  "          "      "  OMe OMe   CH                                        265                                                                               Me CO-n-Pr    CO.sub.2 -n-Pr                                                                        H  OMe OMe   CH                                        266                                                                               "  "          "      "  OMe OMe   N                                         267                                                                               "  "          "      "  OMe Cl    CH                                        268                                                                               "  "          "      Me Me  OMe   N                                         269                                                                               "  "          "      Me OMe OMe   CH                                        270                                                                               Me CO-n-Pr    CO.sub.2 -i-Pr                                                                        H  OMe OMe   CH                                        271                                                                               "  "          "      "  OMe OMe   N                                         272                                                                               "  "          "      "  OMe Me    N                                         273                                                                               "  "          "      "  OMe Cl    CH                                        274                                                                               "  "          "      "  Me  Me    CH                                        275                                                                               "  "          "      "  SMe NEt.sub.2                                                                            N                                         276                                                                               "  "          CO.sub.2 -i-Pr                                                                        Me OMe Me    N                                         277                                                                               "  "          "      Me OMe OMe   CH                                        278                                                                               Me "          CO.sub.2 -Allyl                                                                       H  OMe OMe   CH                                        279                                                                               Et "          CO.sub.2 Me                                                                           H  OMe OMe   CH                                        280                                                                               "  "          "      "  OMe Me    N                                         281                                                                               "  "          "      "  Me  Me    CH                                        282                                                                               "  "          "      "  Cl  OMe   CH                                        283                                                                               "  "          "      Me OMe OMe   CH                                        284                                                                               "  "          "      Me OMe Me    N                                         285                                                                               "  "          CO.sub.2 Et                                                                           H  OMe OMe   CH                                        286                                                                               "  "          "      "  OMe Me    CH                                        287                                                                               "  "          "      "  Cl  OMe   CH                                        288                                                                               "  "          "      "  OMe Me    N                                         289                                                                               "  "          "      Me OMe OMe   CH                                        290                                                                               "  "          "      Me OMe Me    N                                         291                                                                               "  "          CO.sub.2 -n-Pr                                                                        H  OMe OMe   CH                                        292                                                                               "  "          "      "  OMe Me    N                                         293                                                                               "  "          "      "  OMe Cl    CH                                        294                                                                               "  "          "      "  Me  Me    CH                                        295                                                                               "  "          "      Me OMe OMe   CH                                        296                                                                               "  "          "      Me OMe Me    N                                         297                                                                               "  "          CO.sub.2 -i-Pr                                                                        H  OMe OMe   CH                                        298                                                                               "  "          "      "  OMe Me    N                                         299                                                                               n-Pr                                                                              CO-n-Pr    CO.sub.2Me                                                                            H  OMe OMe   CH                                        300                                                                               "  "          "      "  OMe Cl    CH                                        301                                                                               "  "          "      "  Me  Me    CH                                        302                                                                               "  "          "      "  OMe Me    N                                         303                                                                               "  "          "      Me OMe OMe   CH                                        304                                                                               "  "          "      Me OMe Me    N                                         305                                                                               n-Pr                                                                              "          CO.sub.2 Et                                                                           H  OMe Me    N                                         306                                                                               "  "          "      "  OMe OMe   CH                                        307                                                                               "  "          "      "  Me  Me    CH                                        308                                                                               "  "          CO.sub.2 -n-Pr                                                                        "  OMe OMe   CH                                        309                                                                               i-Pr                                                                              "          CO.sub.2 Me                                                                           H  OMe OMe   CH                                        310                                                                               "  "          "      "  OMe Me    N                                         311                                                                               "  "          "      "  Me  Me    CH                                        312                                                                               "  "          "      "  Cl  OMe   N                                         313                                                                               "  "          "      Me OMe Me    N                                         314                                                                               "  "          "      Me OMe OMe   CH                                        315                                                                               Allyl                                                                             "          CO.sub.2Me                                                                            H  OMe OMe   CH                                        316                                                                               "  "          "      "  OMe Cl    CH                                        317                                                                               "  "          "      "  Me  Me    CH                                        318                                                                               "  "          "      "  OMe Me    N                                         319                                                                               "  "          CO.sub.2 Et                                                                           H  OMe OMe   CH                                        320                                                                               "  "          CO.sub.2 -n-Pr                                                                        "  OMe OMe   CH                                        321                                                                               "  "          CO.sub.2 -i-Pr                                                                        "  OMe OMe   CH                                        322                                                                               Me CO-i-Pr    CO.sub.2Me                                                                            H  OMe OMe   CH                                        323                                                                               "  "          "      "  OMe OMe   N                                         324                                                                               "  "          "      "  "   Me    N                                         325                                                                               "  "          "      "  "   "     CH                                        326                                                                               "  "          "      "  NMe.sub.2                                                                          OCH.sub.2 CF.sub.3                                                                   N                                         327                                                                               "  "          "      "  Me  Me    CH                                        328                                                                               "  "          "      "  Me  Me    N                                         329                                                                               "  "          "      "  Cl  OMe   CH                                        330                                                                               "  "          "      Me OMe OMe   CH                                        331                                                                               "  "          "      "  "   Me    N                                         332                                                                               "  "          CO.sub.2Et                                                                            H  OMe OMe   CH                                        333                                                                               "  "          "      "  "   Cl    CH                                        334                                                                               "  "          "      "  Me  Me    CH                                        335                                                                               "  "          "      "  OMe Me    N                                         336                                                                               "  "          "      "  NMe.sub.2                                                                          OCH.sub.2 CF.sub.3                                                                   N                                         337                                                                               "  "          "      Me OMe OMe   CH                                        338                                                                               "  "          "      "  OMe Me    N                                         339                                                                               "  "          CO.sub.2 -n-Pr                                                                        H  OMe OMe   CH                                        340                                                                               "  "          "      "  "   "     N                                         341                                                                               "  "          "      "  OMe Me    N                                         342                                                                               "  "          "      "  Me  Me    CH                                        343                                                                               "  "          "      "  OMe Cl    CH                                        344                                                                               "  "          "      Me Me  OMe   N                                         345                                                                               "  "          "      "  OMe OMe   CH                                        346                                                                               Me CO-i-Pr    CO.sub.2 -i-Pr                                                                        H  OMe OMe   CH                                        347                                                                               "  "          "      "  "   "     N                                         348                                                                               "  "          "      "  OMe Me    N                                         349                                                                               "  "          "      "  OMe Cl    CH                                        350                                                                               "  "          "      "  Me  Me    CH                                        351                                                                               "  "          "      "  SMe NEt.sub.2                                                                            N                                         352                                                                               "  "          CO.sub.2 -i-Pr                                                                        Me OMe Me    N                                         353                                                                               "  "          "      "  OMe OMe   CH                                        354                                                                               Me COCHMe.sub.2                                                                              CH.sub.2 CHCH.sub.2                                                                   H  OMe OMe   CH                                        355                                                                               Et "          CO.sub.2Me                                                                            H  OMe OMe   CH                                        356                                                                               "  "          "      H  OMe Me    N                                         357                                                                               "  "          "      "  Me  Me    CH                                        358                                                                               "  "          "      "  Cl  OMe   CH                                        359                                                                               "  "          "      Me OMe OMe   CH                                        360                                                                               "  "          "      "  OMe Me    N                                         361                                                                               "  "          CO.sub.2Et                                                                            H  OMe OMe   CH                                        362                                                                               "  "          "      "  OMe Me    CH                                        363                                                                               "  "          "      "  Cl  OMe   CH                                        364                                                                               "  "          "      "  OMe Me    N                                         365                                                                               "  "          "      Me OMe OMe   CH                                        366                                                                               "  "          "      "  "   Me    N                                         367                                                                               "  "          CO.sub.2 -n-Pr                                                                        H  OMe OMe   CH                                        368                                                                               "  "          "      "  OMe Me    N                                         369                                                                               "  "          "      "  OMe Cl    CH                                        370                                                                               "  "          "      "  Me  Me    CH                                        371                                                                               "  "          "      Me OMe OMe   CH                                        372                                                                               "  "          "      "  OMe Me    N                                         373                                                                               "  "          CO.sub.2 -i-Pr                                                                        H  OMe OMe   CH                                        374                                                                               "  "          "      "  OMe Me    N                                         375                                                                               "  "          "      "  Me  Me    CH                                        376                                                                               "  "          "      Me OMe Me    N                                         377                                                                               n-Pr                                                                              CO-i-Pr    CO.sub.2Me                                                                            H  OMe OMe   CH                                        378                                                                               "  "          "      "  "   Cl    CH                                        379                                                                               "  "          "      "  Me  Me    CH                                        380                                                                               "  "          "      "  OMe Me    N                                         381                                                                               "  "          "      Me OMe OMe   CH                                        382                                                                               "  "          "      "  OMe Me    N                                         383                                                                               n-Pr                                                                              "          CO.sub.2Et                                                                            H  "   Me    N                                         384                                                                               "  "          "      "  "   OMe   CH                                        385                                                                               "  "          "      "  Me  Me    CH                                        386                                                                               "  "          CO.sub.2 -n-Pr                                                                        "  OMe OMe   CH                                        387                                                                               i-Pr                                                                              "          CO.sub.2Me                                                                            H  OMe OMe   CH                                        388                                                                               "  "          "      "  OMe Me    N                                         389                                                                               "  "          "      "  Me  Me    CH                                        390                                                                               "  "          "      "  Cl  OMe   N                                         391                                                                               "  "          "      Me OMe Me    N                                         392                                                                               "  "          "      "  "   OMe   CH                                        393                                                                               Allyl                                                                             "          CO.sub.2Me                                                                            H  OMe OMe   CH                                        394                                                                               "  "          "      "  "   Cl    CH                                        395                                                                               "  "          "      "  Me  Me    CH                                        396                                                                               "  "          "      "  OMe Me    N                                         397                                                                               "  "          CO.sub.2Et                                                                            H  OMe OMe   CH                                        398                                                                               "  "          CO.sub.2 -n-Pr                                                                        "  OMe OMe   CH                                        399                                                                               "  "          CO.sub.2 -i-Pr                                                                        "  "   "     "                                         400                                                                               Me CO-t-Bu    CO.sub.2Me                                                                            H  OMe OMe   CH                                        401                                                                               "  "          "      "  "   OMe   N                                         402                                                                               "  "          "      "  "   Me    N                                         403                                                                               "  "          "      "  "   "     CH                                        404                                                                               "  "          "      "  NMe.sub.2                                                                          OCH.sub.2 CF.sub.3                                                                   N                                         405                                                                               "  "          "      "  Me  Me    CH                                        406                                                                               "  "          "      "  "   "     N                                         407                                                                               "  "          "      "  Cl  OMe   CH                                        408                                                                               "  "          "      Me OMe OMe   CH                                        409                                                                               "  "          "      "  "   Me    N                                         410                                                                               "  "          CO.sub.2Et                                                                            H  OMe OMe   CH                                        411                                                                               "  "          "      "  "   Cl    CH                                        412                                                                               "  "          "      "  Me  Me    CH                                        413                                                                               "  "          "      "  OMe Me    N                                         414                                                                               "  "          "      "  NMe.sub.2                                                                          OCH.sub.2 CF.sub.3                                                                   N                                         415                                                                               "  "          "      Me OMe OMe   CH                                        416                                                                               "  "          "      "  OMe Me    N                                         417                                                                               "  "          CO.sub.2 -n-Pr                                                                        H  OMe OMe   CH                                        418                                                                               "  "          "      "  "   "     N                                         419                                                                               "  "          "      "  OMe Me    N                                         420                                                                               "  "          "      "  Me  Me    CH                                        421                                                                               "  "          "      "  OMe Cl    CH                                        422                                                                               "  "          "      Me Me  OMe   N                                         423                                                                               "  "          "      "  OMe OMe   CH                                        424                                                                               Me CO-t-Bu    CO.sub.2 -i-Pr                                                                        H  OMe OMe   CH                                        425                                                                               "  "          "      "  "   "     N                                         426                                                                               "  "          "      "  H   Me    N                                         427                                                                               "  "          "      "  OMe Cl    CH                                        428                                                                               "  "          "      "  Me  Me    CH                                        429                                                                               "  "          "      "  SMe NEt.sub.2                                                                            N                                         430                                                                               "  "          CO.sub.2 -i-Pr                                                                        Me OMe Me    N                                         431                                                                               "  "          "      Et OMe OMe   CH                                        432                                                                               Me "          CO.sub.2 -Allyl                                                                       H  OMe OMe   CH                                        433                                                                               Et "          CO.sub.2Me                                                                            H  OMe OMe   CH                                        434                                                                               "  "          "      H  OMe Me    N                                         435                                                                               "  "          "      "  Me  Me    CH                                        436                                                                               "  "          "      "  Cl  OMe   CH                                        437                                                                               "  "          "      Me OMe OMe   CH                                        438                                                                               "  "          "      "  OMe Me    N                                         439                                                                               "  "          CO.sub.2Et                                                                            H  OMe OMe   CH                                        440                                                                               "  "          "      "  OMe Me    CH                                        441                                                                               "  "          "      "  Cl  OMe   CH                                        442                                                                               "  "          "      "  OMe Me    N                                         443                                                                               "  "          "      Me OMe OMe   CH                                        444                                                                               "  "          "      "  "   Me    N                                         445                                                                               "  "          CO.sub.2 -n-Pr                                                                        H  OMe OMe   CH                                        446                                                                               "  "          "      "  OMe Me    N                                         447                                                                               "  "          "      "  OMe Cl    CH                                        448                                                                               "  "          "      "  Me  Me    CH                                        449                                                                               "  "          "      Me OMe OMe   CH                                        450                                                                               "  "          "      "  OMe Me    N                                         451                                                                               "  "          CO.sub.2 -iPr                                                                         H  OMe OMe   CH                                        452                                                                               "  "          "      "  OMe Me    N                                         453                                                                               "  "          "      "  Me  Me    CH                                        454                                                                               "  "          "      Me OMe Me    N                                         455                                                                               n-Pr                                                                              CO-t-Bu    CO.sub.2Me                                                                            H  OMe OMe   CH                                        456                                                                               "  "          "      "  OMe Cl    CH                                        457                                                                               "  "          "      "  Me  Me    CH                                        458                                                                               "  "          "      "  OMe Me    N                                         459                                                                               "  "          "      Me OMe OMe   CH                                        460                                                                               n-Pr                                                                              "          CO.sub.2Et                                                                            Me OMe Me    N                                         461                                                                               n-Pr                                                                              "          CO.sub.2Et                                                                            H  OMe Me    N                                         462                                                                               "  "          "      "  OMe OMe   CH                                        463                                                                               "  "          "      "  Me  Me    CH                                        464                                                                               i-Pr                                                                              "          CO.sub.2Me                                                                            "  OMe OMe   CH                                        465                                                                               i-Pr                                                                              "          "      Me OMe OMe   CH                                        466                                                                               "  "          "      H  OMe Me    N                                         467                                                                               "  "          "      "  Me  Me    CH                                        468                                                                               "  "          "      "  Cl  OMe   N                                         469                                                                               "  "          "      Me OMe Me    N                                         470                                                                               Allyl                                                                             "          "      H  OMe OMe   CH                                        471                                                                               "  "          "      H  OMe Cl    CH                                        472                                                                               "  "          "      "  OMe Me    N                                         473                                                                               "  "          "      "  Me  Me    CH                                        474                                                                               "  "          CO.sub.2Et                                                                            H  OMe OMe   CH                                        475                                                                               "  "          CO.sub.2 -n-Pr                                                                        H  OMe OMe   CH                                        476                                                                               "  "          CO.sub.2 -i-Pr                                                                        H  OMe OMe   CH                                        477                                                                               Me CO-c-Propyl                                                                               CO.sub.2Me                                                                            H  OMe OMe   CH 161° C.                         478                                                                               "  "          "      "  "   OMe   N                                         479                                                                               "  "          "      "  "   Me    N                                         480                                                                               "  "          "      "  "   "     CH                                        481                                                                               "  "          "      "  NMe.sub.2                                                                          OCH.sub.2 CF.sub.3                                                                   N                                         482                                                                               "  "          "      "  Me  Me    CH                                        483                                                                               "  "          "      "  "   "     N                                         484                                                                               "  "          "      "  Cl  OMe   CH                                        485                                                                               "  "          "      Me OMe OMe   CH                                        486                                                                               "  "          "      "  "   Me    N                                         48 "  "          CO.sub.2Et                                                                            H  OMe OMe   CH                                        488                                                                               "  "          "      "  "   Cl    CH                                        489                                                                               "  "          "      "  Me  Me    CH                                        490                                                                               "  "          "      "  OMe Me    N                                         491                                                                               "  "          "      "  NMe.sub.2                                                                          OCH.sub.2 CF.sub.3                                                                   N                                         492                                                                               "  "          "      Me OMe OMe   CH                                        493                                                                               "  "          "      "  OMe Me    N                                         494                                                                               "  "          CO.sub.2 -n-Pr                                                                        H  OMe OMe   CH                                        495                                                                               "  "          "      "  "   "     N                                         496                                                                               "  "          "      "  OMe Me    N                                         497                                                                               "  "          "      "  Me  Me    CH                                        498                                                                               "  "          "      "  OMe Cl    CH                                        499                                                                               "  "          "      Me Me  OMe   N                                         500                                                                               "  "          "      "  OMe OMe   CH                                        501                                                                               Me CO-c-Propyl                                                                               CO.sub.2 -i-Pr                                                                        H  OMe OMe   CH                                        502                                                                               "  "          "      "  "   "     N                                         503                                                                               "  "          "      "  OMe Me    N                                         504                                                                               "  "          "      "  OMe Cl    CH                                        505                                                                               "  "          "      "  Me  Me    CH                                        506                                                                               "  "          "      "  SMe NEt.sub.2                                                                            N                                         507                                                                               "  "          CO.sub.2 -i-Pr                                                                        Me OMe Me    N                                         508                                                                               "  "          "      "  OMe OMe   CH                                        509                                                                               Me "          CO.sub.2 -Allyl                                                                       H  OMe OMe   CH                                        510                                                                               Et "          CO.sub.2Me                                                                            H  OMe OMe   CH                                        511                                                                               "  "          "      H  OMe Me    N                                         512                                                                               "  "          "      "  Me  Me    CH                                        513                                                                               "  "          "      "  Cl  OMe   CH                                        514                                                                               "  "          "      Me OMe OMe   CH                                        515                                                                               "  "          "      "  OMe Me    N                                         516                                                                               "  "          CO.sub.2Et                                                                            H  OMe OMe   CH                                        517                                                                               "  "          "      "  Me  Me    CH                                        518                                                                               "  "          "      "  Cl  OMe   CH                                        519                                                                               "  "          "      "  OMe Me    N                                         520                                                                               "  "          "      Me OMe OMe   CH                                        521                                                                               "  "          "      "  "   Me    N                                         522                                                                               "  "          CO.sub.2 -n-Pr                                                                        H  OMe OMe   CH                                        523                                                                               "  "          "      "  OMe Me    N                                         524                                                                               "  "          "      "  OMe Cl    CH                                        525                                                                               "  "          "      "  Me  Me    CH                                        526                                                                               "  "          "      Me OMe OMe   CH                                        527                                                                               "  "          "      "  OMe Me    N                                         528                                                                               "  "          CO.sub.2 -i-Pr                                                                        H  OMe OMe   CH                                        529                                                                               "  "          "      "  OMe Me    N                                         530                                                                               "  "          "      "  Me  Me    CH                                        531                                                                               "  "          "      Me OMe Me    N                                         532                                                                               n-Pr                                                                              CO-c-Propyl                                                                               CO.sub.2Me                                                                            H  OMe OMe   CH                                        533                                                                               "  "          "      "  "   Cl    CH                                        534                                                                               "  "          "      "  Me  Me    CH                                        535                                                                               "  "          "      "  OMe Me    N                                         536                                                                               "  "          "      Me OMe OMe   CH                                        537                                                                               "  "          "      "  OMe Me    N                                         538                                                                               n-Pr                                                                              "          CO.sub.2Et                                                                            H  "   "     N                                         539                                                                               "  "          "      "  "   OMe   CH                                        540                                                                               "  "          "      "  Me  Me    CH                                        541                                                                               "  "          CO.sub.2 -n-Pr                                                                        "  OMe OMe   CH                                        542                                                                               i-Pr                                                                              "          CO.sub.2Me                                                                            H  OMe OMe   CH                                        543                                                                               "  "          "      "  OMe Me    N                                         544                                                                               "  "          "      "  Me  Me    CH                                        545                                                                               "  "          "      "  Cl  OMe   N                                         546                                                                               "  "          "      Me OMe Me    N                                         547                                                                               "  "          "      "  "   OMe   CH                                        548                                                                               Allyl                                                                             "          CO.sub.2Me                                                                            H  OMe OMe   CH                                        549                                                                               "  "          "      "  "   Cl    CH                                        550                                                                               "  "          "      "  Me  Me    CH                                        551                                                                               "  "          "      "  OMe Me    N                                         552                                                                               "  "          CO.sub.2Et                                                                            H  OMe OMe   CH                                        553                                                                               "  "          CO.sub.2 -n-Pr                                                                        H  OMe OMe   CH                                        554                                                                               "  "          CO.sub.2 -i-Pr                                                                        H  OMe OMe   CH                                        555                                                                               Me CO-n-C.sub.5 H.sub.11                                                                     CO.sub.2Me                                                                            H  OMe OMe   CH                                        556                                                                               "  "          "      "  OMe OMe   N                                         557                                                                               "  "          "      "  "   Me    N                                         558                                                                               "  "          "      "  "   "     CH                                        559                                                                               "  "          "      "  NMe.sub.2                                                                          OCH.sub.2 CF.sub.3                                                                   N                                         560                                                                               "  "          "      "  Me  Me    CH                                        561                                                                               "  "          "      "  "   "     N                                         562                                                                               "  "          "      "  Cl  OMe   CH                                        563                                                                               "  "          "      Me OMe OMe   CH                                        564                                                                               "  "          "      "  "   Me    N                                         565                                                                               "  "          CO.sub.2Et                                                                            H  OMe OMe   CH                                        566                                                                               "  "          "      "  "   Cl    CH                                        567                                                                               "  "          "      "  Me  Me    CH                                        568                                                                               "  "          "      "  OMe Me    N                                         569                                                                               "  "          "      "  NMe.sub.2                                                                          OCH.sub.2 CF.sub.3                                                                   N                                         570                                                                               "  "          "      Me OMe OMe   CH                                        571                                                                               "  "          "      "  OMe Me    N                                         572                                                                               "  "          CO.sub.2 -n-Pr                                                                        H  OMe OMe   CH                                        573                                                                               "  "          "      "  "   "     N                                         574                                                                               "  "          "      "  OMe Me    N                                         575                                                                               "  "          "      "  Me  Me    CH                                        576                                                                               "  "          "      "  OMe Cl    CH                                        577                                                                               "  "          "      Me Me  OMe   N                                         578                                                                               "  "          "      "  OMe OMe   CH                                        579                                                                               Me CO-n-C.sub.5 H.sub.11                                                                     CO.sub.2 -i-Pr                                                                        H  OMe OMe   CH                                        580                                                                               "  "          "      "  "   "     N                                         581                                                                               "  "          "      "  H   Me    N                                         582                                                                               "  "          "      "  OMe Cl    CH                                        583                                                                               "  "          "      "  Me  Me    CH                                        584                                                                               "  "          "      "  SMe NEt.sub.2                                                                            N                                         585                                                                               "  "          CO.sub.2 -i-Pr                                                                        Me OMe Me    N                                         586                                                                               "  "          "      "  OMe OMe   CH                                        587                                                                               Me "          CO.sub.2 -Allyl                                                                       H  OMe OMe   CH                                        588                                                                               Et "          CO.sub.2Me                                                                            H  OMe OMe   CH                                        589                                                                               "  "          "      H  OMe Me    N                                         590                                                                               "  "          "      "  Me  Me    CH                                        591                                                                               "  "          "      "  Cl  OMe   CH                                        592                                                                               "  "          "      Me OMe OMe   CH                                        593                                                                               "  "          "      "  OMe Me    N                                         594                                                                               "  "          CO.sub.2Et                                                                            H  OMe OMe   CH                                        595                                                                               "  "          "      "  OMe Me    CH                                        596                                                                               "  "          "      "  Cl  OMe   CH                                        597                                                                               "  "          "      "  OMe Me    N                                         598                                                                               "  "          "      Me OMe OMe   CH                                        599                                                                               "  "          "      "  "   Me    N                                         600                                                                               "  "          CO.sub.2 -n-Pr                                                                        H  OMe OMe   CH                                        601                                                                               "  "          "      "  OMe Me    N                                         602                                                                               "  "          "      "  OMe Cl    CH                                        603                                                                               "  "          "      "  Me  Me    CH                                        604                                                                               "  "          "      Me OMe OMe   CH                                        605                                                                               "  "          "      "  OMe Me    N                                         606                                                                               "  "          CO.sub.2 -i-Pr                                                                        H  OMe OMe   CH                                        607                                                                               "  "          "      "  OMe Me    N                                         608                                                                               "  "          "      "  Me  Me    CH                                        609                                                                               "  "          "      Me OMe Me    N                                         610                                                                               n-Pr                                                                              CO-n-C.sub.5 H.sub.11                                                                     CO.sub.2Me                                                                            H  OMe OMe   CH                                        611                                                                               "  "          "      "  "   Cl    CH                                        612                                                                               "  "          "      "  Me  Me    CH                                        613                                                                               "  "          "      "  OMe Me    N                                         614                                                                               "  "          "      Me OMe OMe   CH                                        615                                                                               "  "          "      "  OMe Me    N                                         616                                                                               n-Pr                                                                              "          CO.sub.2Et                                                                            H  OMe Me    N                                         617                                                                               "  "          "      "  "   OMe   CH                                        618                                                                               "  "          "      "  Me  Me    CH                                        619                                                                               "  "          CO.sub.2 -n-Pr                                                                        "  OMe OMe   CH                                        620                                                                               i-Pr                                                                              "          CO.sub.2Me                                                                            H  OMe OMe   CH                                        621                                                                               "  "          "      "  OMe Me    N                                         622                                                                               "  "          "      "  Me  Me    CH                                        623                                                                               "  "          "      "  Cl  OMe   N                                         624                                                                               "  "          "         Me  OMe   N                                         625                                                                               "  "          "      "  "   OMe   CH                                        626                                                                               Allyl                                                                             "          CO.sub.2Me                                                                            H  OMe OMe   CH                                        627                                                                               "  "          "      "  "   Cl    CH                                        628                                                                               "  "          "      "  Me  Me    CH                                        629                                                                               "  "          "      "  OMe Me    N                                         630                                                                               "  "          CO.sub.2Et                                                                            H  OMe OMe   CH                                        631                                                                               "  "          CO.sub.2 -n-Pr                                                                        "  "   "     CH                                        632                                                                               "  "          CO.sub.2 -i-Pr                                                                        "  "   "     "                                         633                                                                               Me COCHMeEt   CO.sub.2Me                                                                            H  OMe OMe   CH                                        634                                                                               "  "          "      "  "   OMe   N                                         635                                                                               "  "          "      "  "   Me    N                                         636                                                                               "  "          "      "  "   "     CH                                        637                                                                               "  "          "      "  NMe.sub.2                                                                          OCH.sub.2 CF.sub.3                                                                   N                                         638                                                                               "  "          "      "  Me  Me    CH                                        639                                                                               "  "          "      "  "   "     N                                         640                                                                               "  "          "      "  Cl  OMe   CH                                        641                                                                               "  "          "      Me OMe OMe   CH                                        642                                                                               "  "          "      "  "   Me    N                                         643                                                                               "  "          CO.sub.2Et                                                                            H  OMe OMe   CH                                        644                                                                               "  "          "      "  "   Cl    CH                                        645                                                                               "  "          "      "  Me  Me    CH                                        646                                                                               "  "          "      "  OMe Me    N                                         647                                                                               "  "          "      "  NMe.sub.2                                                                          OCH.sub.2 CF.sub.3                                                                   N                                         648                                                                               "  "          "      Me OMe OMe   CH                                        649                                                                               "  "          "      "  OMe Me    N                                         650                                                                               "  "          CO.sub.2 -n-Pr                                                                        H  OMe OMe   CH                                        651                                                                               "  "          "      "  "   "     N                                         652                                                                               "  "          "      "  OMe Me    N                                         653                                                                               "  "          "      "  Me  Me    CH                                        654                                                                               "  "          "      "  OMe Cl    CH                                        655                                                                               "  "          "      Me Me  OMe   N                                         656                                                                               "  "          "      "  OMe OMe   CH                                        657                                                                               Me COCHMeEt   CO.sub.2 -i-Pr                                                                        H  OMe OMe   CH                                        658                                                                               "  "          "      "  "   "     N                                         659                                                                               "  "          "      "  OMe Me    N                                         660                                                                               "  "          "      "  OMe Cl    CH                                        661                                                                               "  "          "      "  Me  Me    CH                                        662                                                                               "  "          "      "  SMe NEt.sub.2                                                                            N                                         663                                                                               "  "          CO.sub.2 -i-Pr                                                                        Me OMe Me    N                                         664                                                                               "  "          "      "  OMe OMe   CH                                        665                                                                               Me "          CO.sub.2 -Allyl                                                                       H  OMe OMe   CH                                        666                                                                               Et "          CO.sub.2Me                                                                            H  OMe OMe   CH                                        667                                                                               "  "          "      H  OMe Me    N                                         668                                                                               "  "          "      "  Me  Me    CH                                        669                                                                               "  "          "      "  Cl  OMe   CH                                        670                                                                               "  "          "      Me OMe OMe   CH                                        671                                                                               "  "          "      "  OMe Me    N                                         672                                                                               "  "          CO.sub.2Et                                                                            H  OMe OMe   CH                                        673                                                                               "  "          "      "  OMe Me    CH                                        674                                                                               "  "          "      "  Cl  OMe   CH                                        675                                                                               "  "          "      "  OMe Me    N                                         676                                                                               "  "          "      Me OMe OMe   CH                                        677                                                                               "  "          "      "  "   Me    N                                         678                                                                               "  "          CO.sub.2 -n-Pr                                                                        H  OMe OMe   CH                                        679                                                                               "  "          "      "  OMe Me    N                                         680                                                                               "  "          "      "  OMe Cl    CH                                        681                                                                               "  "          "      "  Me  Me    CH                                        682                                                                               "  "          "      Me OMe OMe   CH                                        683                                                                               "  "          "      "  OMe Me    N                                         684                                                                               "  "          CO.sub.2 -i-Pr                                                                        H  OMe OMe   CH                                        685                                                                               "  "          "      "  OMe Me    N                                         686                                                                               "  "          "      "  Me  Me    CH                                        687                                                                               "  "          "      Me OMe Me    N                                         688                                                                               n-Pr                                                                              COCHMeEt   CO.sub.2Me                                                                            H  OMe OMe   CH                                        689                                                                               "  "          "      "  "   Cl    CH                                        690                                                                               "  "          "      "  Me  Me    CH                                        691                                                                               "  "          "      "  OMe Me    N                                         692                                                                               "  "          "      Me OMe OMe   CH                                        693                                                                               "  "          "      "  OMe Me    N                                         694                                                                               n-Pr                                                                              "          CO.sub.2Et                                                                            H  "   "     N                                         695                                                                               "  "          "      "  "   OMe   CH                                        696                                                                               "  "          "      "  Me  Me    CH                                        697                                                                               "  "          CO.sub.2 -n-Pr                                                                        "  OMe OMe   CH                                        698                                                                               i-Pr                                                                              "          CO.sub.2Me                                                                            H  OMe OMe   CH                                        699                                                                               "  "          "      "  OMe Me    N                                         700                                                                               "  "          "      "  Me  Me    CH                                        701                                                                               "  "          "      "  Cl  OMe   N                                         702                                                                               "  "          "      Me OMe Me    N                                         703                                                                               "  "          "      "  "   OMe   CH                                        704                                                                               Allyl                                                                             "          CO.sub.2Me                                                                            H  OMe OMe   CH                                        705                                                                               "  "          "      "  "   Cl    CH                                        706                                                                               "  "          "      "  Me  Me    CH                                        707                                                                               "  "          "      "  OMe Me    N                                         708                                                                               "  "          CO.sub.2Et                                                                            H  OMe OMe   CH                                        709                                                                               "  "          CO.sub.2 -n-Pr                                                                        "  "   "     CH                                        710                                                                               "  "          CO.sub.2 -i-Pr                                                                        "  "   "     CH                                        711                                                                               Me                                                                                 ##STR13## CO.sub.2Me                                                                            H  OMe OMe   CH                                        712                                                                               "  "          "      "  OMe OMe   N                                         713                                                                               "  "          "      "  "   Me    N                                         714                                                                               "  "          "      "  "   "     CH                                        715                                                                               "  "          "      "  NMe.sub.2                                                                          OCH.sub.2 CF.sub.3                                                                   N                                         716                                                                               "  "          "      "  Me  Me    CH                                        717                                                                               "  "          "      "  "   "     N                                         718                                                                               "  "          "      "  Cl  OMe   CH                                        719                                                                               "  "          "      Me OMe OMe   CH                                        720                                                                               "  "          "      "  "   Me    N                                         721                                                                               "  "          CO.sub.2Et                                                                            H  OMe OMe   CH                                        722                                                                               "  "          "      "  "   Cl    CH                                        723                                                                               "  "          "      "  Me  Me    CH                                        724                                                                               "  "          "      "  OMe Me    N                                         725                                                                               "  "          "      "  NMe.sub.2                                                                          OCH.sub.2 CF.sub.3                                                                   N                                         726                                                                               "  "          "      Me OMe OMe   CH                                        727                                                                               "  "          "      "  OMe Me    N                                         728                                                                               "  "          CO.sub.2 -n-Pr                                                                        H  OMe OMe   CH                                        729                                                                               "  "          "      "  "   "     N                                         730                                                                               "  "          "      "  OMe Me    N                                         731                                                                               "  "          "      "  Me  Me    CH                                        732                                                                               "  "          "      "  OMe Cl    CH                                        733                                                                               "  "          "      Me Me  OMe   N                                         734                                                                               "  "          "      "  OMe OMe   CH                                        735                                                                               Me                                                                                 ##STR14## CO.sub.2 -i-Pr                                                                        H  OMe OMe   CH                                        736                                                                               "  "          "      "  "   "     N                                         737                                                                               "  "          "      "  OMe Me    N                                         738                                                                               "  "          "      "  OMe Cl    CH                                        739                                                                               "  "          "      "  Me  Me    CH                                        740                                                                               "  "          "      "  SMe NEt.sub.2                                                                            N                                         741                                                                               "  "          CO.sub.2 -i-Pr                                                                        Me OMe Me    N                                         742                                                                               "  "          "      "  OMe OMe   CH                                        743                                                                               Me "          CO.sub.2 -Allyl                                                                       H  OMe OMe   CH                                        744                                                                               Et "          CO.sub.2Me                                                                            H  OMe OMe   CH                                        745                                                                               "  "          "      H  OMe Me    N                                         746                                                                               "  "          "      "  Me  Me    CH                                        747                                                                               "  "          "      "  Cl  OMe   CH                                        748                                                                               "  "          "      Me OMe OMe   CH                                        749                                                                               "  "          "      "  OMe Me    N                                         750                                                                               "  "          CO.sub.2Et                                                                            H  OMe OMe   CH                                        751                                                                               "  "          "      "  OMe Me    CH                                        752                                                                               "  "          "      "  Cl  OMe   CH                                        753                                                                               "  "          "      "  OMe Me    N                                         754                                                                               "  "          "      Me OMe OMe   CH                                        755                                                                               "  "          "      "  "   Me    N                                         756                                                                               "  "          CO.sub.2 -n-Pr                                                                        H  OMe OMe   CH                                        757                                                                               "  "          "      "  OMe Me    N                                         758                                                                               "  "          "      "  OMe Cl    CH                                        759                                                                               "  "          "      "  Me  Me    CH                                        760                                                                               "  "          "      Me OMe OMe   CH                                        761                                                                               "  "          "      "  OMe Me    N                                         762                                                                               "  "          CO.sub.2 -i-Pr                                                                        H  OMe OMe   CH                                        763                                                                               "  "          "      "  OMe Me    N                                         764                                                                               "  "          "      "  Me  Me    CH                                        765                                                                               "  "          "      Me OMe Me    N                                         766                                                                               n-Pr                                                                               ##STR15## CO.sub.2Me                                                                            H  OMe OMe   CH                                        767                                                                               "  "          "      "  "   Cl    CH                                        768                                                                               "  "          "      "  Me  Me    CH                                        769                                                                               "  "          "      "  OMe Me    N                                         770                                                                               "  "          "      Me OMe OMe   CH                                        771                                                                               "  "          "      "  OMe Me    N                                         772                                                                               n-Pr                                                                              "          CO.sub.2Et                                                                            H  OMe OMe   N                                         773                                                                               "  "          "      "  "   OMe   CH                                        774                                                                               "  "          "      "  Me  Me    CH                                        775                                                                               "  "          CO.sub.2 -n-Pr                                                                        "  OMe OMe   CH                                        776                                                                               i-Pr                                                                              "          CO.sub.2Me                                                                            H  OMe OMe   CH                                        777                                                                               "  "          "      "  OMe Me    N                                         778                                                                               "  "          "      "  Me  Me    CH                                        779                                                                               "  "          "      "  Cl  OMe   N                                         780                                                                               "  "          "      Me OMe Me    N                                         781                                                                               "  "          "      "  "   OMe   CH                                        782                                                                               Allyl                                                                             "          CO.sub.2Me                                                                            H  OMe OMe   CH                                        783                                                                               "  "          "      "  Cl  CH                                              784                                                                               "  "          "      "  Me  Me    CH                                        785                                                                               "  "          "      "  OMe Me    N                                         786                                                                               "  "          CO.sub.2Et                                                                            H  OMe OMe   CH                                        787                                                                               "  "          CO.sub.2 -n-Pr                                                                        "  "   "     "                                         788                                                                               "  "          CO.sub.2 -i-pr                                                                        "  "   "     "                                         789                                                                               Me                                                                                 ##STR16## CO.sub.2 Me                                                                           H  OMe OMe   CH                                        790                                                                               "  "          "      "  "   OMe   N                                         791                                                                               "  "          "      "  "   Me    N                                         792                                                                               "  "          "      "  "   "     CH                                        793                                                                               "  "          "      "  NMe.sub.2                                                                          OCH.sub.2 CF.sub.3                                                                   N                                         794                                                                               "  "          "      "  Me  Me    CH                                        795                                                                               "  "          "      "  "   "     N                                         796                                                                               "  "          "      "  Cl  OMe   CH                                        797                                                                               "  "          "      Me OMe OMe   CH                                        798                                                                               "  "          "      "  "   Me    N                                         799                                                                               "  "          CO.sub.2Et                                                                            H  OMe OMe   CH                                        800                                                                               "  "          "      "  "   Cl    CH                                        801                                                                               "  "          "      "  Me  Me    CH                                        802                                                                               "  "          "      "  OMe Me    N                                         803                                                                               "  "          "      "  NMe.sub.2                                                                          OCH.sub.2 CF.sub.3                                                                   N                                         804                                                                               "  "          "      Me OMe OMe   CH                                        805                                                                               "  "          "      "  OMe Me    N                                         806                                                                               "  "          CO.sub.2 -n-Pr                                                                        H  OMe OMe   CH                                        807                                                                               "  "          "      "  "   "     N                                         808                                                                               "  "          "      "  OMe Me    N                                         809                                                                               "  "          "      "  Me  Me    CH                                        810                                                                               "  "          "      "  OMe Cl    CH                                        811                                                                               "  "          "      Me Me  OMe   N                                         812                                                                               "  "          "      "  OMe OMe   CH                                        813                                                                               Me "          CO.sub.2 -i-Pr                                                                        H  OMe OMe   CH                                        814                                                                               "  "          "      "  "   "     N                                         815                                                                               "  "          "      "  OMe Me    N                                         816                                                                               "  "          "      "  OMe Cl    CH                                        817                                                                               "  "          "      "  Me  Me    CH                                        818                                                                               "  "          "      "  SMe NEt.sub.2                                                                            N                                         819                                                                               "  "          CO.sub.2 -i-Pr                                                                        Me OMe Me    N                                         820                                                                               "  "          "      "  OMe OMe   CH                                        821                                                                               Me "          CO.sub.2 -Allyl                                                                       H  OMe OMe   CH                                        822                                                                               Et "          CO.sub.2Me                                                                            H  OMe OMe   CH                                        823                                                                               "  "          "      H  OMe Me    N                                         824                                                                               "  "          "      "  Me  Me    CH                                        825                                                                               "  "          "      "  Cl  OMe   CH                                        826                                                                               "  "          "      Me OMe OMe   CH                                        827                                                                               "  "          "      "  OMe Me    N                                         828                                                                               "  "          CO.sub.2Et                                                                            H  OMe OMe   CH                                        829                                                                               "  "          "      "  OMe Me    CH                                        830                                                                               "  "          "      "  Cl  OMe   CH                                        831                                                                               "  "          "      "  OMe Me    N                                         832                                                                               "  "          "      Me OMe OMe   CH                                        833                                                                               "  "          "      "  "   Me    N                                         834                                                                               "  "          CO.sub.2 -n-Pr                                                                        H  OMe OMe   CH                                        835                                                                               "  "          "      "  OMe Me    N                                         836                                                                               "  "          "      "  OMe Cl    CH                                        837                                                                               "  "          "      "  Me  Me    CH                                        838                                                                               "  "          "      Me OMe OMe   CH                                        839                                                                               "  "          "      "  OMe Me    N                                         840                                                                               "  "          CO.sub.2 -i-Pr                                                                        H  OMe OMe   CH                                        841                                                                               "  "          "      "  OMe Me    N                                         842                                                                               "  "          "      "  Me  Me    CH                                        843                                                                               "  "          "      Me OMe Me    N                                         844                                                                               n-Pr                                                                              "          CO.sub.2Me                                                                            H  OMe OMe   CH                                        845                                                                               "  "          "      "  "   Cl    CH                                        846                                                                               "  "          "      "  Me  Me    CH                                        847                                                                               "  "          "      "  OMe Me    N                                         848                                                                               "  "          "      Me OMe OMe   CH                                        849                                                                               "  "          "      "  OMe Me    N                                         850                                                                               n-Pr                                                                              "          CO.sub.2Et                                                                            H  "   "     N                                         851                                                                               "  "          "      "  "   OMe   CH                                        852                                                                               "  "          "      "  Me  Me    CH                                        853                                                                               "  "          CO.sub.2 -n-Pr                                                                        "  OMe OMe   CH                                        854                                                                               i-Pr                                                                              "          CO.sub.2Me                                                                            H  OMe OMe   CH                                        855                                                                               "  "          "      "  OMe Me    N                                         856                                                                               "  "          "      "  Me  Me    CH                                        857                                                                               "  "          "      "  Cl  OMe   N                                         858                                                                               "  "          "      Me OMe Me    N                                         859                                                                               "  "          "      "  "   OMe   CH                                        860                                                                               Allyl                                                                             "          CO.sub.2Me                                                                            H  OMe OMe   CH                                        861                                                                               "  "          "      "  "   Cl    CH                                        862                                                                               "  "          "      "  Me  Me    CH                                        863                                                                               "  "          "      "  OMe Me    N                                         864                                                                               "  "          CO.sub.2Et                                                                            H  OMe OMe   CH                                        865                                                                               "  "          CO.sub.2 -n-Pr                                                                        H  OMe OMe   CH                                        __________________________________________________________________________

    __________________________________________________________________________     No.                                                                               R.sup.1                                                                            R.sup.2    R.sup.3                                                                              R.sup.4                                                                            X     Y      Z      m.p.                           __________________________________________________________________________     866                                                                               "   "          CO.sub.2 -i-Pr                                                                       "   "     "      CH                                    867                                                                               Me                                                                                  ##STR17## CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    868                                                                               "   "          "     "   "     OMe    N                                     869                                                                               "   "          "     "   "     Me     N                                     870                                                                               "   "          "     "   "     "      CH                                    871                                                                               "   "          "     "   NMe.sub.2                                                                            OCH.sub.2 CF.sub.3                                                                    N                                     872                                                                               "   "          "     "   Me    Me     CH                                    873                                                                               "   "          "     "   "     Cl     N                                     874                                                                               "   "          "     "   Cl    OMe    CH                                    875                                                                               "   "          "     Me  OMe   OMe    CH                                    876                                                                               "   "          "     "   "     Me     N                                     877                                                                               "   "          CO.sub.2 Et                                                                          H   OMe   OMe    CH                                    878                                                                               "   "          "     "   "     Cl     CH                                    879                                                                               "   "          "     "   Me    Me     CH                                    880                                                                               "   "          "     "   OMe   Me     N                                     881                                                                               "   "          "     "   NMe.sub.2                                                                            OCH.sub.2 CF.sub.3                                                                    N                                     882                                                                               "   "          "     Me  OMe   OMe    CH                                    883                                                                               "   "          "     "   OMe   Me     N                                     884                                                                               "   "          CO.sub.2 -n-Pr                                                                       H   OMe   OMe    CH                                    885                                                                               "   "          "     "   "     "      N                                     886                                                                               "   "          "     "   OMe   Me     N                                     887                                                                               "   "          "     "   Me    Me     CH                                    888                                                                               "   "          "     "   OMe   Cl     CH                                    889                                                                               "   "          "     Me  Me    OMe    N                                     890                                                                               "   "          "     "   OMe   OMe    CH                                    891                                                                               Me  "          CO.sub.2 -i-Pr                                                                       H   OMe   OMe    CH                                    892                                                                               "   "          "     "   "     "      N                                     893                                                                               "   "          "     "   H     Me     N                                     894                                                                               "   "          "     "   OMe   Cl     CH                                    895                                                                               "   "          "     "   Me    Me     CH                                    896                                                                               "   "          "     "   SMe   NEt.sub.2                                                                             N                                     897                                                                               "   "          CO.sub.2 -i-Pr                                                                       Me  OMe   Me     N                                     898                                                                               "   "          "     "   OMe   OMe    CH                                    899                                                                               Me  "          CO.sub.2 -Allyl                                                                      H   OMe   OMe    CH                                    900                                                                               Et  "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    901                                                                               "   "          "     H   OMe   Me     N                                     902                                                                               "   "          "     "   Me    Me     CH                                    903                                                                               "   "          "     "   Cl    OMe    CH                                    904                                                                               "   "          "     Me  OMe   OMe    CH                                    905                                                                               "   "          "     "   OMe   Me     N                                     906                                                                               "   "          CO.sub.2 Et                                                                          H   OMe   OMe    CH                                    907                                                                               "   "          "     "   OMe   Me     CH                                    908                                                                               "   "          "     "   Cl    OMe    CH                                    909                                                                               "   "          "     "   OMe   Me     N                                     910                                                                               "   "          "     Me  OMe   OMe    CH                                    911                                                                               "   "          "     "   "     Me     N                                     912                                                                               "   "          CO.sub.2 -n-Pr                                                                       H   OMe   OMe    CH                                    913                                                                               "   "          "     "   OMe   Me     N                                     914                                                                               "   "          "     "   OMe   Cl     CH                                    915                                                                               "   "          "     "   Me    Me     CH                                    916                                                                               "   "          "     Me  OMe   OMe    CH                                    917                                                                               "   "          "     "   OMe   Me     N                                     918                                                                               "   "          CO.sub.2 -i-Pr                                                                       H   OMe   OMe    CH                                    919                                                                               "   "          "     "   OMe   Me     N                                     920                                                                               "   "          "     "   Me    Me     CH                                    921                                                                               "   "          "     Me  OMe   Me     N                                     922                                                                               n-Pr                                                                               "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    923                                                                               "   "          "     "   "     Cl     CH                                    924                                                                               "   "          "     "   Me    Me     CH                                    925                                                                               "   "          "     "   OMe   Me     N                                     926                                                                               "   "          "     Me  OMe   OMe    CH                                    927                                                                               "   "          "     "   OMe   Me     N                                     928                                                                               n-Pr                                                                               "          CO.sub.2 Et                                                                          H   "     "      N                                     929                                                                               "   "          "     "   "     OMe    CH                                    930                                                                               "   "          "     "   Me    Me     CH                                    931                                                                               "   "          CO.sub.2 -n-Pr                                                                       "   OMe   OMe    CH                                    932                                                                               i-Pr                                                                               "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    933                                                                               "   "          "     "   OMe   Me     N                                     934                                                                               "   "          "     "   Me    Me     CH                                    935                                                                               "   "          "     "   Cl    OMe    N                                     936                                                                               "   "          "     Me  OMe   Me     N                                     937                                                                               "   "          "     "   "     OMe    CH                                    938                                                                               Allyl                                                                              "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    939                                                                               "   "          "     "   "     Cl     CH                                    940                                                                               "   "          "     "   Me    Me     CH                                    941                                                                               "   "          "     "   OMe   Me     N                                     942                                                                               "   "          CO.sub.2 Et                                                                          H   OMe   OMe    CH                                    943                                                                               "   "          CO.sub.2 -n-Pr                                                                       "   "     "      CH                                    944                                                                               "   "          CO.sub.2 -i-Pr                                                                       "   "     "      "                                     945                                                                               Me                                                                                  ##STR18## CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    946                                                                               "   "          "     "   "     OMe    N                                     947                                                                               "   "          "     "   "     Me     N                                     948                                                                               "   "          "     "   "     "      CH                                    949                                                                               "   "          "     "   NMe.sub.2                                                                            OCH.sub.2 CF.sub.3                                                                    N                                     950                                                                               "   "          "     "   Me    Me     CH                                    951                                                                               "   "          "     "   "     "      N                                     952                                                                               "   "          "     "   Cl    OMe    CH                                    953                                                                               "   "          "     Me  OMe   OMe    CH                                    954                                                                               "   "          "     "   "     Me     N                                     955                                                                               "   "          CO.sub.2 Et                                                                          H   OMe   OMe    CH                                    956                                                                               "   "          "     "   "     Cl     CH                                    957                                                                               "   "          "     "   Me    Me     CH                                    958                                                                               "   "          "     "   OMe   Me     N                                     959                                                                               "   "          "     "   NMe.sub.2                                                                            OCH.sub.2 CF.sub.3                                                                    N                                     960                                                                               "   "          "     Me  OMe   OMO    CH                                    961                                                                               "   "          "     "   OMe   Me     N                                     962                                                                               "   "          CO.sub.2 -n-Pr                                                                       H   OMe   OMe    CH                                    963                                                                               "   "          "     "   "     "      N                                     964                                                                               "   "          "     "   OMe   Me     N                                     965                                                                               "   "          "     "   Me    Me     CH                                    966                                                                               "   "          "     "   OMe   Cl     CH                                    967                                                                               "   "          "     Me  Me    OMe    N                                     968                                                                               "   "          "     "   OMe   OMe    CH                                    969                                                                               Me                                                                                  ##STR19## CO.sub.2 -i-Pr                                                                       H   OMe   OMe    CH                                    970                                                                               "   "          "     "   "     "      N                                     971                                                                               "   "          "     "   H     Me     N                                     972                                                                               "   "          "     "   OMe   Cl     CH                                    973                                                                               "   "          "     "   Me    Me     CH                                    974                                                                               "   "          "     "   SMe   NEt.sub.2                                                                             N                                     975                                                                               "   "          CO.sub.2 -i-Pr                                                                       Me  OMe   Me     N                                     976                                                                               "   "          "     "   OMe   OMe    CH                                    977                                                                               Me  "          CO.sub.2 -Allyl                                                                      H   OMe   OMe    CH                                    978                                                                               Et  "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    979                                                                               "   "          "     H   OMe   Me     N                                     980                                                                               "   "          "     "   Me    Me     CH                                    981                                                                               "   "          "     "   Cl    OMe    CH                                    982                                                                               "   "          "     Me  OMe   OMe    CH                                    983                                                                               "   "          "     "   OMe   Me     N                                     984                                                                               "   "          CO.sub.2 Et                                                                          H   OMe   OMe    CH                                    985                                                                               "   "          "     "   OMe   Me     CH                                    986                                                                               "   "          "     "   Cl    OMe    CH                                    987                                                                               "   "          "     "   OMe   Me     N                                     988                                                                               "   "          "     Me  OMe   OMe    CH                                    989                                                                               "   "          "     "   "     Me     N                                     990                                                                               "   "          CO.sub.2 -n-Pr                                                                       H   OMe   OMe    CH                                    991                                                                               "   "          "     "   OMe   Me     N                                     992                                                                               "   "          "     "   OMe   Cl     CH                                    993                                                                               "   "          "     "   Me    Me     CH                                    994                                                                               "   "          "     Me  OMO   OMe    CH                                    995                                                                               "   "          "     "   OMO   Me     N                                     996                                                                               "   "          CO.sub.2 -i-Pr                                                                       H   OMe   OMe    CH                                    997                                                                               "   "          "     "   OMe   Me     N                                     998                                                                               "   "          "     "   Me    Me     CH                                    999                                                                               "   "          "     Me  OMe   Me     N                                     1.000                                                                             n-Pr                                                                               "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.001                                                                             "   "          "     "   "     Cl     CH                                    1.002                                                                             "   "          "     "   Me    Me     CH                                    1.003                                                                             "   "          "     "   OMe   Me     N                                     1.004                                                                             "   "          "     Me  OMe   OMe    CH                                    1.005                                                                             "   "          "     "   OMe   Me     N                                     1.006                                                                             n-Pr                                                                               "          CO.sub.2 Et                                                                          H   "     "      N                                     1.007                                                                             "   "          "     "   Cl    OMe    CH                                    1.008                                                                             "   "          "     "   Me    Me     CH                                    1.009                                                                             "   "          CO.sub.2 -n-Pr                                                                           OMe   OMe    CH                                    1.010                                                                             i-Pr                                                                               "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.011                                                                             "   "          "     "   OMe   Me     N                                     1.012                                                                             "   "          "     "   Me    Me     CH                                    1.013                                                                             "   "          "     "   Cl    OMe    N                                     1.014                                                                             "   "          "     Me  OMe   Me     N                                     1.015                                                                             "   "          "     "   "     OMe    CH                                    1.016                                                                             Allyl                                                                              "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.017                                                                             "   "          "     "   "     Cl     CH                                    1.018                                                                             "   "          "     "   Me    Me     CH                                    1.019                                                                             "   "          "     "   OMe   Me     N                                     1.020                                                                             "   "          CO.sub.2 Et                                                                          H   OMe   OMe    CH                                    1.021                                                                             "   "          CO.sub.2 -n-Pr                                                                       "   "     "      CH                                    1.022                                                                             "   "          CO.sub.2 -i-Pr                                                                       "   "     "      CH                                    1.023                                                                             Me  COPh       CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.024                                                                             "   "          "     "   "     OMe    N                                     1.025                                                                             "   "          "     "   "     Me     N                                     1.026                                                                             "   "          "     "   OMe   "      CH                                    1.027                                                                             "   "          "     "   NMe.sub.2                                                                            OCH.sub.2 CF.sub.3                                                                    N                                     1.028                                                                             "   "          "     "   Me    Me     CH                                    1.029                                                                             "   "          "     "   "     "      N                                     1.030                                                                             "   "          "     "   Cl    OMO    CH                                    1.031                                                                             "   "          "     Me  OMe   OMe    CH                                    1.032                                                                             "   "          "     "   "     Me     N                                     1.033                                                                             "   "          CO.sub.2 Et                                                                          H   OMe   OMe    CH                                    1.034                                                                             "   "          "     "   "     Cl     CH                                    1.035                                                                             "   "          "     "   Me    Me     CH                                    1.036                                                                             "   "          "     "   OMe   Me     N                                     1.037                                                                             "   "          "     "   NMe.sub.2                                                                            OCH.sub.2 CF.sub.3                                                                    N                                     1.038                                                                             "   "          "     Me  OMe   OMe    CH                                    1.039                                                                             "   "          "     "   OMe   Me     N                                     1.040                                                                             "   "          CO.sub.2 -n-Pr                                                                       H   OMe   OMe    CH                                    1.041                                                                             "   "          "     "   "     "      N                                     1.042                                                                             "   "          "     "   OMe   Me     N                                     1.043                                                                             "   "          "     "   Me    Me     CH                                    1.044                                                                             "   "          "     "   OMe   Cl     CH                                    1.045                                                                             "   "          "     Me  Me    OMe    N                                     1.046                                                                             "   "          "     "   OMe   OMO    CH                                    1.047                                                                             Me  COPh       CO.sub.2 -i-Pr                                                                       OMe OMe   OMe    CH                                    1.048                                                                             "   "          "     "   "     "      N                                     1.049                                                                             "   "          "     "   OMe   Me     N                                     1.050                                                                             "   "          "     "   OMe   Cl     CH                                    1.051                                                                             "   "          "     "   Me    Me     CH                                    1.052                                                                             "   "          "     "   SMe   NEt.sub.2                                                                             N                                     1.053                                                                             "   "          CO.sub.2 -i-Pr                                                                       Me  OMe   Me     N                                     1.054                                                                             "   "          "     "   OMe   OMe    CH                                    1.055                                                                             Me  "          CO.sub.2 -Allyl                                                                      H   OMe   OMe    CH                                    1.056                                                                             Et  "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.057                                                                             "   "          "     H   OMe   Me     N                                     1.058                                                                             "   "          "     "   Me    Me     CH                                    1.059                                                                             "   "          "     "   Cl    OMe    CH                                    1.060                                                                             "   "          "     Me  OMe   OMe    CH                                    1.061                                                                             "   "          "     "   OMe   Me     N                                     1.062                                                                             "   "          CO.sub.2 Et                                                                          H   OMe   OMe    CH                                    1.063                                                                             "   "          "     "   OMe   Me     CH                                    1.064                                                                             "   "          "     "   Cl    OMe    CH                                    1.065                                                                             "   "          "     "   OMe   Me     N                                     1.066                                                                             "   "          "     Me  OMe   OMe    CH                                    1.067                                                                             "   "          "     "   "     Me     N                                     1.068                                                                             "   "          CO.sub.2 -n-Pr                                                                       H   OMe   OMe    CH                                    1.069                                                                             "   "          "     "   OMe   Me     N                                     1.070                                                                             "   "          "     "   OMe   Cl     CH                                    1.071                                                                             "   "          "     "   Me    Me     CH                                    1.072                                                                             "   "          "     Me  OMe   OMe    CH                                    1.073                                                                             "   "          "     "   OMe   Me     N                                     1.074                                                                             "   "          CO.sub.2 -i-Pr                                                                       H   OMe   OMe    CH                                    1.075                                                                             "   "          "     "   OMe   Me     N                                     1.076                                                                             "   "          "     Me  OMe   Me     N                                     1.077                                                                             n-Pr                                                                               COPh       CO.sub.2 Me                                                                          H   OMe   OMO    CH                                    1.078                                                                             "   "          "     "   "     Cl     CH                                    1.079                                                                             "   "          "     "   Me    Me     CH                                    1.080                                                                             "   "          "     "   OMe   Me     N                                     1.081                                                                             "   "          "     Me  OMe   OMe    CH                                    1.082                                                                             "   "          "     "   OMe   Me     N                                     1.083                                                                             n-Pr                                                                               "          CO.sub.2 Et                                                                          H   "     "      N                                     1.084                                                                             "   "          "     "   "     OMe    CH                                    1.085                                                                             "   "          "     "   Me    Me     CH                                    1.086                                                                             "   "          CO.sub.2 -n-Pr                                                                       "   OMe   OMe    CH                                    1.087                                                                             i-Pr                                                                               "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.088                                                                             "   "          "     "   OMe   Me     N                                     1.089                                                                             "   "          "     "   Me    Me     CH                                    1.090                                                                             "   "          "     "   Cl    OMe    N                                     1.091                                                                             "   "          "     Me  OMe   Me     N                                     1.092                                                                             "   "          "     "   "     OMe    CH                                    1.093                                                                             Allyl                                                                              "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.094                                                                             "   "          "     "   "     Cl     CH                                    1.095                                                                             "   "          "     "   Me    Me     CH                                    1.096                                                                             "   "          "     "   OMe   Me     N                                     1.097                                                                             "   "          CO.sub.2 Et                                                                          H   OMe   OMe    CH                                    1.098                                                                             "   "          CO.sub.2 -n-Pr                                                                       H   OMe   OMe    CH                                    1.099                                                                             "   "          CO.sub.2 -i-Pr                                                                       "   "     "      CH                                    1.100                                                                             Me                                                                                  ##STR20## CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.101                                                                             "   "          "     "   "     OMe    N                                     1.102                                                                             "   "          "     "   "     Me     N                                     1.103                                                                             "   "          "     "   "     "      CH                                    1.104                                                                             "   "          "     "   NMe.sub.2                                                                            OCH.sub.2 CF.sub.3                                                                    N                                     1.105                                                                             "   "          "     "   Me    Me     CH                                    1.106                                                                             "   "          "     "   "     "      N                                     1.107                                                                             "   "          "     "   Cl    OMe    CH                                    1.108                                                                             "   "          "     Me  OMe   OMe    CH                                    1.109                                                                             "   "          "     "   "     Me     N                                     1.110                                                                             "   "          CO.sub.2 -El                                                                         H   OMe   OMe    CH                                    1.111                                                                             "   "          "     "   "     Cl     CH                                    1.112                                                                             "   "          "     "   Me    Me     CH                                    1.113                                                                             "   "          "     "   OMe   Me     N                                     1.114                                                                             "   "          "     "   NMe.sub.2                                                                            OCH.sub.2 CF.sub.3                                                                    N                                     1.115                                                                             "   "          "     Me  OMe   OMe    CH                                    1.116                                                                             "   "          "     "   OMe   Me     N                                     1.117                                                                             "   "          CO.sub.2 -n-Pr                                                                       H   OMe   OMe    CH                                    1.118                                                                             "   "          "     "   "     "      N                                     1.119                                                                             "   "          "     "   OMe   Me     N                                     1.120                                                                             "   "          "     "   Me    Me     CH                                    1.121                                                                             "   "          "     "   OMe   Cl     CH                                    1.122                                                                             "   "          "     Me  Me    OMe    N                                     1.123                                                                             "   "          "     "   OMe   OMe    CH                                    1.124                                                                             Me  "          CO.sub.2 -i-PT                                                                       H   OMe   OMe    CH                                    1.125                                                                             "   "          "     "   "     "      N                                     1.126                                                                             "   "          "     "   H     Me     N                                     1.127                                                                             "   "          "     "   OMe   Cl     CH                                    1.128                                                                             "   "          "     "   Me    Me     CH                                    1.129                                                                             "   "          "     "   SMe   NEt.sub.2                                                                             N                                     1.130                                                                             "   "          CO.sub.2 -i-Pr                                                                       Me  OMe   Me     N                                     1.131                                                                             "   "          "     "   OMe   OMe    CH                                    1.132                                                                             Me  "          CO.sub.2 -Allyl                                                                      H   OMe   OMO    CH                                    1.133                                                                             Et  "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.134                                                                             "   "          "     H   OMe   Me     N                                     1.135                                                                             "   "          "     "   Me    Me     CH                                    1.136                                                                             "   "          "     "   Cl    OMe    CH                                    1.137                                                                             "   "          "     Me  OMe   OMe    CH                                    1.138                                                                             "   "          "     "   OMe   Me     N                                     1.139                                                                             "   "          CO.sub.2 Et                                                                          H   OMe   OMe    CH                                    1.140                                                                             "   "          "     "   OMe   Me     CH                                    1.141                                                                             "   "          "     "   Cl    OMe    CH                                    1.142                                                                             "   "          "     "   OMe   Me     N                                     1.143                                                                             "   "          "     Me  OMe   OMe    CH                                    1.144                                                                             "   "          "     "   "     Me     N                                     1.145                                                                             "   "          CO.sub.2 -n-Pr                                                                       H   OMe   OMe    CH                                    1.146                                                                             "   "          "     "   OMe   Me     N                                     1.147                                                                             "   "          "     "   OMe   Cl     CH                                    1.148                                                                             "   "          "     "   Me    Me     CH                                    1.149                                                                             "   "          "     Me  OMe   OMe    CH                                    1.150                                                                             "   "          "     Me  OMe   Me     N                                     1.151                                                                             "   "          CO.sub.2 -i-Pr                                                                       H   OMe   OMS    CH                                    1.152                                                                             "   "          "     "   OMe   Me     N                                     1.153                                                                             "   "          "     "   Me    Me     CH                                    1.154                                                                             "   "          "     Me  OMe   Me     N                                     1.155                                                                             n-Pr                                                                                ##STR21## CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.156                                                                             "   "          "     "   "     Cl     CH                                    1.157                                                                             "   "          "     "   Me    Me     cm                                    1.158                                                                             "   "          "     "   OMe   Me     N                                     1.159                                                                             "   "          "     Me  OMe   OMe    CH                                    1.160                                                                             "   "          "     "   OMe   Me     N                                     1.161                                                                             n-Pr                                                                               "          CO.sub.2 Et                                                                          H   OMe   Me     N                                     1.162                                                                             "   "          "     "   "     OMe    CH                                    1.163                                                                             "   "          "     "   Me    Me     CH                                    1.164                                                                             "   "          CO.sub.2 -n-Pr                                                                       "   OMe   OMe    CH                                    1.165                                                                             i-Pr                                                                               "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.166                                                                             "   "          "     "   OMe   Me     N                                     1.167                                                                             "   "          "     "   Me    Me     CH                                    1.168                                                                             "   "          "     "   Cl    OMe    N                                     1.169                                                                             "   "          "     Me  OMe   Me     N                                     1.170                                                                             "   "          "     "   "     OMe    CH                                    1.171                                                                             Allyl                                                                              "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.172                                                                             "   "          "     "   "     Cl     CH                                    1.173                                                                             "   "          "     "   Me    Me     CH                                    1.174                                                                             "   "          "     "   OMe   Me     N                                     1.175                                                                             "   "          CO.sub.2 -Et                                                                         H   OMe   OMe    CH                                    1.176                                                                             "   "          CO.sub.2 -n-Pr                                                                       "   OMe   OMe    CH                                    1.177                                                                             "   "          CO.sub.2 -i-pr                                                                       H   OMe   OMe    CH                                    1.178                                                                             Me  COOMe      CO.sub.2 -M8                                                                         H   OMe   OMS    CH     128° C.                 1.179                                                                             "   "          "     "   "     OMe    N                                     1.180                                                                             "   "          "     "   "     Me     N      s. Bsp. o)                     1.181                                                                             "   "          "     "   "     "      CH     89-101                         1.182                                                                             "   "          "     "   NM3.sub.2                                                                            OCH.sub.2 CF.sub.3                                                                    N                                     1.183                                                                             "   "          "     "   Me    Me     CH     s. Bsp. m)                     1.184                                                                             "   "          "     "   "     "      N                                     1.185                                                                             "   "          "     "   Cl    OMe    CH     s. Bsp. n)                     1.186                                                                             "   "          "     Me  OMe   OMe    CH     150-154                        1.187                                                                             "   "          "     "   "     Me     N                                     1.188                                                                             "   "          CO.sub.2 Et                                                                          H   OMe   OMe    CH                                    1.189                                                                             "   "          "     "   "     Cl     CH                                    1.190                                                                             "   "          "     "   Me    Me     CH                                    1.191                                                                             "   "          "     "   OMe   Me     N                                     1.192                                                                             "   "          "     "   NMe.sub.2                                                                            OCH.sub.2 CF.sub.3                                                                    N                                     1.193                                                                             "   "          "     Me  OMe   OMe    CH                                    1.194                                                                             "   "          "     "   OMe   Me     N                                     1.195                                                                             "   "          CO.sub.2 -n-Pr                                                                       H   OMe   OMe    CH                                    1.196                                                                             "   "          "     "   "     "      N                                     1.197                                                                             "   "          "     "   OMe   Me     N                                     1.198                                                                             "   "          "     "   Me    Me     CH                                    1.199                                                                             "   "          "     "   OMe   Cl     CH                                    1.200                                                                             "   "          "     Me  Me    OMe    N                                     1.201                                                                             "   "          "     "   OMe   OMe    CH                                    1.202                                                                             Me  COOMe      CO.sub.2 -i-Pr                                                                       H   OMe   OMe    CH                                    1.203                                                                             "   "          "     "   "     "      N                                     1.204                                                                             "   "          "     "   OMe   Me     N                                     1.205                                                                             "   "          "     "   OMe   Cl     CH                                    1.206                                                                             "   "          "     "   Me    Me     CH                                    1.207                                                                             "   "          "     "   SMe   NEt.sub.2                                                                             N                                     1.208                                                                             "   "          CO.sub.2 -i-Pr                                                                       Me  OMe   Me     N                                     1.209                                                                             "   "          "     "   OMe   OMe    CH                                    1.210                                                                             Me  "          CO.sub.2 -Allyl                                                                      H   OMe   OMe    CH                                    1.211                                                                             Et  "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.212                                                                             "   "          "     H   OMe   Me     N                                     1.213                                                                             "   "          "     "   Me    Me     CH                                    1.214                                                                             "   "          "     "   Cl    OMS    CH                                    1.215                                                                             "   "          "     Me  OMe   OMe    CH                                    1.216                                                                             "   "          "     "   OMe   Me     N                                     1.217                                                                             "   "          CO.sub. 2 Et                                                                         H   OMe   OMe    CH                                    1.218                                                                             "   "          "     "   OMe   Me     CH                                    1.219                                                                             "   "          "     "   Cl    OMe    CH                                    1.220                                                                             "   "          "     "   OMe   Me     N                                     1.221                                                                             "   "          "     Me  OMe   OMe    CH                                    1.222                                                                             "   "          "     "   "     Me     N                                     1.223                                                                             "   "          CO.sub.2 -n-Pr                                                                       H   OMe   OMe    CH                                    1.224                                                                             "   "          "     "   OMe   Me     N                                     1.225                                                                             "   "          "     "   OMe   Cl     CH                                    1.226                                                                             "   "          "     "   Me    Me     CH                                    1.227                                                                             "   "          "     Me  OMe   OMe    CH                                    1.228                                                                             "   "          "     "   OMe   Me     N                                     1.229                                                                             "   "          CO.sub.2 -i-Pr                                                                       H   OMe   OMe    CH                                    1.230                                                                             "   "          "     "   OMe   Me     N                                     1.231                                                                             "   "          "     "   Me    Me     CH                                    1.232                                                                             "   "          "     Me  OMe   Me     N                                     1.233                                                                             n-Pr                                                                               COOMe      CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.234                                                                             "   "          "     "   "     Cl     CH                                    1.235                                                                             "   "          "     "   Me    Me     CH                                    1.236                                                                             "   "          "     "   OMe   Me     N                                     1.237                                                                             "   "          "     Me  OMe   OMe    CH                                    1.238                                                                             "   "          "     "   OMe   Me     N                                     1.239                                                                             n-Pr                                                                               "          CO.sub.2 Et                                                                          H   OMe   Me     N                                     1.240                                                                             "   "          "     "   "     OMe    CH                                    1.241                                                                             "   "          "     "   Me    Me     CH                                    1.242                                                                             "   "          CO.sub.2 -n-Pr                                                                       "   OMe   OMe    CH                                    1.243                                                                             i-Pr                                                                               "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.244                                                                             "   "          "     "   OMe   Me     N                                     1.245                                                                             "   "          "     "   Me    Me     CH                                    1.246                                                                             "   "          "     "   Cl    OMe    N                                     1.247                                                                             "   "          "     Me  OMe   Me     N                                     1.248                                                                             "   "          "     "   "     OMe    CH                                    1.249                                                                             Allyl                                                                              "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.250                                                                             "   "          "     "   "     Cl     CH                                    1.251                                                                             "   "          "     "   Me    Me     CH                                    1.252                                                                             "   "          "     "   OMe   Me     N                                     1.253                                                                             "   "          CO.sub.2 Et                                                                          H   OMe   OMe    CH                                    1.254                                                                             "   "          CO.sub.2 -n-Pr                                                                       "   "     "      "                                     1.255                                                                             "   "          CO.sub.2 -i-Pr                                                                       "   "     "      CH                                    1.256                                                                             Me  COOEt      CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.257                                                                             "   "          "     "   "     OMe    N                                     1.258                                                                             "   "          "     "   "     Me     N                                     1.259                                                                             "   "          "     "   "     "      CH                                    1.260                                                                             "   "          "     "   NMe.sub.2                                                                            OCH.sub.2 CF.sub.3                                                                    N                                     1.261                                                                             "   "          "     "   Me    Me     CH                                    1.262                                                                             "   "          "     "   "     "      N                                     1.263                                                                             "   "          "     "   Cl    OMe    CH                                    1.264                                                                             "   "          "     Me  OMe   OMe    CH                                    1.265                                                                             "   "          "     "   "     Me     N                                     1.266                                                                             "   "          CO.sub.2 Et                                                                          H   OMe   OMe    CH                                    1.267                                                                             "   "          "     "   "     Cl     CH                                    1.268                                                                             "   "          "     "   Me    Me     CH                                    1.269                                                                             "   "          "     "   OMe   Me     N                                     1.270                                                                             "   "          "     "   NMe.sub.2                                                                            OCH.sub.2 CF.sub.3                                                                    N                                     1.271                                                                             "   "          "     Me  OMe   OMe    CH                                    1.272                                                                             "   "          "     "   OMe   Me     N                                     1.273                                                                             "   "          CO.sub.2 -n-Pr                                                                       H   OMe   OMe    CH                                    1.274                                                                             "   "          "     "   "     "      N                                     1.275                                                                             "   "          "     "   OMe   Me     N                                     1.276                                                                             "   "          "     "   Me    Me     CH                                    1.277                                                                             "   "          "     "   OMe   Cl     CH                                    1.278                                                                             "   "          "     Me  Me    OMe    N                                     1.279                                                                             "   "          "     "   OMe   OMe    CH                                    1.280                                                                             Me  COOEt      CO.sub.2 -i-Pr                                                                       H   OMe   OMe    CH                                    1.281                                                                             "   "          "     "   "     "      N                                     1.282                                                                             "   "          "     "   OMe   Me     N                                     1.283                                                                             "   "          "     "   OMe   Cl     CH                                    1.284                                                                             "   "          "     "   Me    Me     CH                                    1.285                                                                             "   "          "     "   SMe   NEt.sub.2                                                                             N                                     1.286                                                                             "   "          CO.sub.2 -i-Pr                                                                       Me  OMe   Me     N                                     1.287                                                                             "   "          "     "   OMe   OMe    CH                                    1.288                                                                             Me  "          CO.sub.2 -Allyl                                                                      H   OMe   OMe    CH                                    1.289                                                                             Et  "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.290                                                                             "   "          "     H   OMe   Me     N                                     1.291                                                                             "   "          "     "   Me    Me     CH                                    1.292                                                                             "   "          "     "   Cl    OMe    CH                                    1.293                                                                             "   "          "     Me  OMe   OMe    CH                                    1.294                                                                             "   "          "     "   OMe   Me     N                                     1.295                                                                             "   "          CO.sub.2 Et                                                                          H   OMe   OMe    CH                                    1.296                                                                             "   "          "     "   OMe   Me     CH                                    1.297                                                                             "   "          "     "   Cl    OMe    CH                                    1.298                                                                             "   "          "     "   OMe   Me     N                                     1.299                                                                             "   "          "     Me  OMe   OMe    CH                                    1.300                                                                             "   "          "     "   "     Me     N                                     1.301                                                                             "   "          CO.sub.2 -n-Pr                                                                       H   OMe   OMe    CH                                    1.302                                                                             "   "          "     "   OMe   Me     N                                     1.303                                                                             "   "          "     "   OMe   Cl     CH                                    1.304                                                                             "   "          "     "   Me    Me     CH                                    1.305                                                                             "   "          "     Me  OMe   OMe    CH                                    1.306                                                                             "   "          "     "   OMe   Me     N                                     1.307                                                                             "   "          CO.sub.2 -i-Pr                                                                       H   OMe   OMe    CH                                    1.308                                                                             "   "          "     "   OMe   Me     N                                     1.309                                                                             "   "          "     "   Me    Me     CH                                    1.310                                                                             "   "          "     Me  OMe   Me     N                                     1.311                                                                             n-Pr                                                                               CO.OEt     CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.312                                                                             "   "          "     "   "     Cl     CH                                    1.313                                                                             "   "          "     "   Me    Me     CH                                    1.314                                                                             "   "          "     "   OMe   Me     N                                     1.315                                                                             "   "          "     Me  OMe   OMe    CH                                    1.316                                                                             "   "          "     "   OMe   Me     N                                     1.317                                                                             n-Pr                                                                               "          CO.sub.2 Et                                                                          H   "     "      N                                     1.318                                                                             "   "          "     "   "     OMe    CH                                    1.319                                                                             "   "          "     "   Me    Me     CH                                    1.320                                                                             "   "          CO.sub.2 -n-Pr                                                                       "   OMe   OMe    CH                                    1.321                                                                             i-Pr                                                                               "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.322                                                                             "   "          "     "   OMe   Me     N                                     1.323                                                                             "   "          "     "   Me    Me     CH                                    1.324                                                                             "   "          "     "   Cl    OMe    N                                     1.325                                                                             "   "          "     Me  OMe   Me     N                                     1.326                                                                             "   "          "     "   "     OMe    CH                                    1.327                                                                             Allyl                                                                              "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.328                                                                             "   "          "     "   "     Cl     CH                                    1.329                                                                             "   "          "     "   Me    Me     CH                                    1.330                                                                             "   "          "     "   OMe   Me     N                                     1.331                                                                             "   "          CO.sub.2 Et                                                                          H   OMe   OMe    CH                                    1.332                                                                             "   "          CO.sub.2 -n-Pr                                                                       H   OMe   OMe    CH                                    1.333                                                                             "   "          CO.sub.2 -i-Pr                                                                       "   "     "      "                                     1.334                                                                             Me  COO-i-Pr   CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.335                                                                             "   "          "     "   "     OMe    N                                     1.336                                                                             "   "          "     "   "     Me     N                                     1.337                                                                             "   "          "     "   "     "      CH                                    1.338                                                                             "   "          "     "   NMe.sub.2                                                                            OCH.sub.2 CF.sub.3                                                                    N                                     1.339                                                                             "   "          "     "   Me    Me     CH                                    1.340                                                                             "   "          "     "   "     "      N                                     1.341                                                                             "   "          "     "   Cl    OMe    CH                                    1.342                                                                             "   "          "     Me  OMe   OMe    CH                                    1.343                                                                             "   "          "     "   "     Me     N                                     1.344                                                                             "   "          CO.sub.2 Et                                                                          H   OMe   OMe    CH                                    1.345                                                                             "   "          "     "   "     Cl     CH                                    1.346                                                                             "   "          "     "   Me    Me     CH                                    1.347                                                                             "   "          "     "   OMe   Me     N                                     1.348                                                                             "   "          "     "   NMe.sub.2                                                                            OCH.sub.2 CF.sub.3 N                         1.349                                                                             "   "          "     Me  OMe   OMe    CH                                    1.350                                                                             "   "          "     "   OMe   Me     N                                     1.351                                                                             "   "          CO.sub.2 -n-Pr                                                                       H   OMe   OMe    CH                                    1.352                                                                             "   "          "     "   "     "      N                                     1.353                                                                             "   "          "     "   OMe   Me     N                                     1.354                                                                             "   "          "     "   Me    Me     CH                                    1.355                                                                             "   "          "     "   OMe   Cl     CH                                    1.356                                                                             "   "          "     Me  Me    OMe    N                                     1.357                                                                             "   "          "     "   OMe   OMe    CH                                    1.358                                                                             Me  COO-i-Pr   CO.sub.2 -i-Pr                                                                       H   OMe   OMe    CH                                    1.359                                                                             "   "          "     "   "     "      N                                     1.360                                                                             "   "          "     "   H     Me     N                                     1.361                                                                             "   "          "     "   OMe   Cl     CH                                    1.362                                                                             "   "          "     "   Me    Me     CH                                    1.363                                                                             "   "          "     "   SMe   NEt.sub.2                                                                             N                                     1.364                                                                             "   "          CO.sub.2 -i-Pr                                                                       Me  OMe   Me     N                                     1.365                                                                             "   "          "     "   OMe   OMe    CH                                    1.366                                                                             Me  "          CO.sub.2 -Allyl                                                                      H   OMe   OMe    CH                                    1.367                                                                             Et  "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.368                                                                             "   "          "     H   OMe   Me     N                                     1.369                                                                             "   "          "     "   Me    Me     CH                                    1.370                                                                             "   "          "     "   Cl    OMe    CH                                    1.371                                                                             "   "          "     Me  OMe   OMe    CH                                    1.372                                                                             "   "          "     "   OMe   Me     N                                     1.373                                                                             "   "          CO.sub.2 Et                                                                          H   OMe   OMe    CH                                    1.374                                                                             "   "          "     "   OMe   Me     CH                                    1.375                                                                             "   "          "     "   Cl    OMe    CH                                    1.376                                                                             "   "          "     "   OMe   Me     N                                     1.377                                                                             "   "          "     Me  OMe   OMe    CH                                    1.378                                                                             "   "          "     "   "     Me     N                                     1.379                                                                             "   "          CO.sub.2 -n-Pr                                                                       H   OMe   OMe    CH                                    1.380                                                                             "   "          "     "   OMe   Me     N                                     1.381                                                                             "   "          "     "   OMe   Cl     CH                                    1.382                                                                             "   "          "     "   Me    Me     CH                                    1.383                                                                             "   "          "     Me  OMe   OMe    CH                                    1.384                                                                             "   "          "     "   OMe   Me     N                                     1.385                                                                             "   "          CO.sub.2 -i-Pr                                                                       H   OMe   OMe    CH                                    1.386                                                                             "   "          "     "   OMe   Me     N                                     1.387                                                                             "   "          "     "   Me    Me     CH                                    1.388                                                                             "   "          "     Me  OMe   Me     N                                     1.389                                                                             n-Pr                                                                               COO-i-Pr   CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.390                                                                             "   "          "     "   "     Cl     CH                                    1.391                                                                             "   "          "     "   Me    Me     CH                                    1.392                                                                             "   "          "     "   OMe   Me     N                                     1.393                                                                             "   "          "     Me  OMe   OMe    CH                                    1.394                                                                             "   "          "     "   OMe   Me     N                                     1.395                                                                             n-Pr                                                                               "          CO.sub.2 Et                                                                          H   "     "      N                                     1.396                                                                             "   "          "     "   "     OMe    CH                                    1.397                                                                             "   "          "     "   Me    Me     CH                                    1.398                                                                             "   "          CO.sub.2 -n-Pr                                                                       "   OMe   OMe    CH                                    1.399                                                                             i-Pr                                                                               "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.400                                                                             "   "          "     "   OMe   Me     N                                     1.401                                                                             "   "          "     "   Me    Me     CH                                    1.402                                                                             "   "          "     "   Cl    OMe    N                                     1.403                                                                             "   "          "     Me  OMe   Me     N                                     1.404                                                                             "   "          "     "   "     OMe    CH                                    1.405                                                                             Allyl                                                                              "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.406                                                                             "   "          "     "   "     Cl     CH                                    1.407                                                                             "   "          "     "   Me    Me     CH                                    1.408                                                                             "   "          "     "   OMe   Me     N                                     1.409                                                                             "   "          CO.sub.2 Et                                                                          H   OMe   OMe    CH                                    1.410                                                                             "   "          CO.sub.2 -n-Pr                                                                       "   "     "      CH                                    1.411                                                                             "   "          CO.sub.2 -i-Pr                                                                       "   "     "      CH                                    1.412                                                                             Me  COO-n-Pr   CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.413                                                                             "   "          "     "   "     OMe    N                                     1.414                                                                             "   "          "     "   "     Me     N                                     1.415                                                                             "   "          "     "   "     "      CH                                    1.416                                                                             "   "          "     "   NMe.sub.2                                                                            OCH.sub.2 CF.sub.3                                                                    N                                     1.417                                                                             "   "          "     "   Me    Me     CH                                    1.418                                                                             "   "          "     "   "     "      N                                     1.419                                                                             "   "          "     "   Cl    OMe    CH                                    1.420                                                                             "   "          "     Me  OMe   OMe    CH                                    1.421                                                                             "   "          "     "   "     Me     N                                     1.422                                                                             "   "          CO.sub.2 Et                                                                          H   OMe   OMe    CH                                    1.423                                                                             "   "          "     "   "     Cl     CH                                    1.424                                                                             "   "          "     "   Me    Me     CH                                    1.425                                                                             "   "          "     "   OMe   Me     N                                     1.426                                                                             "   "          "     "   NMe.sub.2                                                                            OCH.sub.2 CF.sub.3                                                                    N                                     1.427                                                                             "   "          "     Me  OMe   OMe    CH                                    1.428                                                                             "   "          "     "   OMe   Me     N                                     1.429                                                                             "   "          CO.sub.2 -n-Pr                                                                       H   OMe   OMe    CH                                    1.430                                                                             "   "          "     "   "     "      N                                     1.431                                                                             "   "          "     "   OMe   Me     N                                     1.432                                                                             "   "          "     "   Me    Me     CH                                    1.433                                                                             "   "          "     "   OMe   Cl     CH                                    1.434                                                                             "   "          "     Me  Me    OMe    N                                     1.435                                                                             "   "          "     "   OMe   OMe    CH                                    1.436                                                                             Me  COO-n-Pr   CO.sub.2 -i-Pr                                                                       H   OMe   OMe    CH                                    1.437                                                                             "   "          "     "   "     "      N                                     1.438                                                                             "   "          "     "   OMe   Me     N                                     1.439                                                                             "   "          "     "   OMe   Cl     CH                                    1.440                                                                             "   "          "     "   Me    Me     CH                                    1.441                                                                             "   "          "     "   SMe   NEt.sub.2                                                                             N                                     1.442                                                                             "   "          CO.sub.2 -i-Pr                                                                       Me  OMe   Me     N                                     1.443                                                                             "   "          "     "   OMe   OMe    CH                                    1.444                                                                             Me  "          CO.sub.2 -Allyi                                                                      H   OMe   OMe    CH                                    1.445                                                                             Et  "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.446                                                                             "   "          "     H   OMe   Me     N                                     1.447                                                                             "   "          "     "   Me    Me     CH                                    1.448                                                                             "   "          "     "   Cl    OMe    CH                                    1.449                                                                             "   "          "     Me  OMe   OMe    CH                                    1.450                                                                             "   "          "     "   OMe   Me     N                                     1.451                                                                             "   "          CO.sub.2 Et                                                                          H   OMe   OMe    CH                                    1.452                                                                             "   "          "     "   OMe   Me     CH                                    1.453                                                                             "   "          "     "   Cl    OMe    CH                                    1.454                                                                             "   "          "     "   OMe   Me     N                                     1.455                                                                             "   "          "     Me  OMe   OMe    CH                                    1.456                                                                             "   "          "     "   "     Me     N                                     1.457                                                                             "   "          CO.sub.2 -n-Pr                                                                       H   OMe   OMe    CH                                    1.458                                                                             "   "          "     "   OMe   Me     N                                     1.459                                                                             "   "          "     "   OMe   Cl     CH                                    1.460                                                                             "   "          "     "   Me    Me     CH                                    1.461                                                                             "   "          "     Me  OMe   OMe    CH                                    1.462                                                                             "   "          "     "   OMe   Me     N                                     1.463                                                                             "   "          CO.sub.2 -i-Pr                                                                       H   OMe   OMe    CH                                    1.464                                                                             "   "          "     "   OMe   Me     N                                     1.465                                                                             "   "          "     "   Me    Me     CH                                    1.466                                                                             "   "          "     Me  OMe   Me     N                                     1.467                                                                             n-Pr                                                                               COO-n-Pr   CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.468                                                                             "   "          "     "   "     Cl     CH                                    1.469                                                                             "   "          "     "   Me    Me     CH                                    1.470                                                                             "   "          "     "   OMe   Me     N                                     1.471                                                                             "   "          "     Me  OMe   OMe    CH                                    1.472                                                                             "   "          "     "   OMe   Me     N                                     1.473                                                                             n-Pr                                                                               "          CO.sub. 2 Et                                                                         H   "     "      N                                     1.474                                                                             "   "          "     "   "     OMe    CH                                    1.475                                                                             "   "          "     "   Me    Me     CH                                    1.476                                                                             "   "          CO.sub.2 -n-Pr                                                                       "   OMe   OMe    CH                                    1.477                                                                             i-Pr                                                                               "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.478                                                                             "   "          "     "   OMe   Me     N                                     1.479                                                                             "   "          "     "   Me    Me     CH                                    1.480                                                                             "   "          "     "   Cl    OMe    N                                     1.481                                                                             "   "          "     Me  OMe   Me     N                                     1.482                                                                             "   "          "     "   "     OMe    CH                                    1.483                                                                             Allyl                                                                              "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.484                                                                             "   "          "     "   "     Cl     CH                                    1.485                                                                             "   "          "     "   Me    Me     CH                                    1.486                                                                             "   "          "     "   OMe   Me     N                                     1.487                                                                             "   "          CO.sub.2 Et                                                                          H   OMe   OMe    CH                                    1.488                                                                             "   "          CO.sub.2 -n-Pr                                                                       "   "     "      CH                                    1.489                                                                             "   "          CO.sub.2 -i-Pr                                                                       "   "     "      CH                                    1.490                                                                             Me  COO-allyl  CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.491                                                                             "   "          "     "   "     OMe    N                                     1.492                                                                             "   "          "     "   "     Me     N                                     1.493                                                                             "   "          "     "   "     "      CH                                    1.494                                                                             "   "          "     "   NMe.sub.2                                                                            OCH.sub.2 CF.sub.3                                                                    N                                     1.495                                                                             "   "          "     "   Me    Me     CH                                    1.496                                                                             "   "          "     "   "     "      N                                     1.497                                                                             "   "          "     "   Cl    OMe    CH                                    1.498                                                                             "   "          "     Me  OMe   OMe    CH                                    1.499                                                                             "   "          "     "   "     Me     N                                     1.500                                                                             "   "          CO.sub.2 Et                                                                          H   OMe   OMe    CH                                    1.501                                                                             "   "          "     "   "     Cl     CH                                    1.502                                                                             "   "          "     "   Me    Me     CH                                    1.503                                                                             "   "          "     "   OMe   Me     N                                     1.504                                                                             "   "          "     "   NMe.sub.2                                                                            OCH.sub.2 CF.sub.3                                                                    N                                     1.505                                                                             "   "          "     Me  OMe   OMe    CH                                    1.506                                                                             "   "          "     "   OMe   Me     N                                     1.507                                                                             "   "          CO.sub.2 -n-Pr                                                                       H   OMe   OMe    CH                                    1.508                                                                             "   "          "     "   "     "      N                                     1.509                                                                             "   "          "     "   OMe   Me     N                                     1.510                                                                             "   "          "     "   Me    Me     CH                                    1.511                                                                             "   "          "     "   OMe   Cl     CH                                    1.512                                                                             "   "          "     Me  Me    OMe    N                                     1.513                                                                             "   "          "     "   OMe   OMe    CH                                    1.514                                                                             Me  COO-allyl  CO.sub.2 -i-Pr                                                                       H   OMe   OMe    CH                                    1.515                                                                             "   "          "     "   "     "      N                                     1.516                                                                             "   "          "     "   H     Me     N                                     1.517                                                                             "   "          "     "   OMe   Cl     CH                                    1.518                                                                             "   "          "     "   Me    Me     CH                                    1.519                                                                             "   "          "     "   SMe   NEt.sub.2                                                                             N                                     1.520                                                                             "   "          CO.sub.2 -i-Pr                                                                       Me  OMe   Me     N                                     1.521                                                                             "   "          "     "   OMe   OMe    CH                                    1.522                                                                             Me  "          CO.sub.2 -Allyl                                                                      H   OMe   OMe    CH                                    1.523                                                                             Et  "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.524                                                                             "   "          "     H   OMe   Me     N                                     1.525                                                                             "   "          "     "   Me    Me     CH                                    1.526                                                                             "   "          "     "   Cl    OMe    CH                                    1.527                                                                             "   "          "     Me  OMe   OMe    CH                                    1.528                                                                             "   "          "     "   OMe   Me     N                                     1.529                                                                             "   "          CO.sub.2 Et                                                                          H   OMe   OMe    CH                                    1.530                                                                             "   "          "     "   OMG   Me     CH                                    1.531                                                                             "   "          "     "   Cl    OMe    CH                                    1.532                                                                             "   "          "     "   OMe   Me     N                                     1.533                                                                             "   "          "     Me  OMe   OMe    CH                                    1.534                                                                             "   "          "     "   "     Me     N                                     1.535                                                                             "   "          CO.sub.2 -n-Pr                                                                       H   OMe   OMe    CH                                    1.536                                                                             "   "          "     "   OMe   Me     N                                     1.537                                                                             "   "          "     "   OMe   Cl     CH                                    1.538                                                                             "   "          "     "   Me    Me     CH                                    1.539                                                                             "   "          "     Me  OMe   OMe    CH                                    1.540                                                                             "   "          "     "   OMe   Me     N                                     1.541                                                                             "   "          CO.sub.2 -i-Pr                                                                       H   OMe   OMe    CH                                    1.542                                                                             "   "          "     "   OMe   Me     N                                     1.543                                                                             "   "          "     "   Me    Me     CH                                    1.544                                                                             "   "          "     Me  OMe   Me     N                                     1.545                                                                             n-Pr                                                                               COO-allyl  CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.546                                                                             "   "          "     "   "     Cl     CH                                    1.547                                                                             "   "          "     "   Me    Me     CH                                    1.548                                                                             "   "          "     "   OMe   Me     N                                     1.549                                                                             "   "          "     Me  OMe   OMe    CH                                    1.550                                                                             "   "          "     "   OMe   Me     N                                     1.551                                                                             n-Pr                                                                               "          CO.sub.2 Et                                                                          H   "     "      N                                     1.552                                                                             "   "          "     "   "     OMe    CH                                    1.553                                                                             "   "          "     "   Me    Me     CH                                    1.554                                                                             "   "          CO.sub.2 -n-Pr                                                                       "   OMe   OMe    CH                                    1.555                                                                             i-Pr                                                                               "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.556                                                                             "   "          "     "   OMe   Me     N                                     1.557                                                                             "   "          "     "   Me    Me     CH                                    1.558                                                                             "   "          "     "   Cl    OMe    N                                     1.559                                                                             "   "          "     Me  OMe   Me     N                                     1.560                                                                             "   "          "     "   "     OMe    CH                                    1.561                                                                             Allyl                                                                              "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.562                                                                             "   "          "     "   "     Cl     CH                                    1.563                                                                             "   "          "     "   Me    Me     CH                                    1.564                                                                             "   "          "     "   OMe   Me     N                                     1.565                                                                             "   "          CO.sub.2 Et                                                                          H   OMe   OMe    CH                                    1.565                                                                             "   "          CO.sub.2 -n-Pr                                                                       "   "     "      CH                                    1.567                                                                             "   "          CO.sub.2 -i-Pr                                                                       "   "     "      CH                                    1.568                                                                             Me  CONHEt     CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.569                                                                             "   "          "     "   "     OMe    N                                     1.570                                                                             "   "          "     "   "     Me     N                                     1.571                                                                             "   "          "     "   "     "      CH                                    1.572                                                                             "   "          "     "   NMe.sub.2                                                                            OCH.sub.2 CF.sub.3                                                                    N                                     1.573                                                                             "   "          "     "   Me    Me     CH                                    1.574                                                                             "   "          "     "   "     "      N                                     1.575                                                                             "   "          "     "   Cl    OMe    CH                                    1.576                                                                             "   "          "     Me  OMe   OMe    CH                                    1.577                                                                             "   "          "     "   "     Me     N                                     1.578                                                                             "   "          CO.sub.2 Et                                                                          H   OMe   OMe    CH                                    1.579                                                                             "   "          "     "   "     Cl     CH                                    1.580                                                                             "   "          "     "   Me    Me     CH                                    1.581                                                                             "   "          "     "   OMe   Me     N                                     1.582                                                                             "   "          "     "   NMe.sub.2                                                                            OCH.sub.2 CF.sub.3                                                                    N                                     1.583                                                                             "   "          "     Me  OMe   OMe    CH                                    1.584                                                                             "   "          "     "   OMe   Me     N                                     1.585                                                                             "   "          CO.sub.2 -n-Pr                                                                       H   OMe   OMe    CH                                    1.586                                                                             "   "          "     "   "     "      N                                     1.587                                                                             "   "          "     "   OMe   Me     N                                     1.588                                                                             "   "          "     "   Me    Me     CH                                    1.589                                                                             "   "          "     "   OMe   Cl     CH                                    1.590                                                                             "   "          "     Me  Me    OMe    N                                     1.591                                                                             "   "          "     "   OMe   OMe    CH                                    1.592                                                                             Me  CO NHEt    CO.sub.2 -i-Pr                                                                       H   OMe   OMe    CH                                    1.593                                                                             "   "          "     "   "     "      N                                     1.594                                                                             "   "          "     "   OMe   Me     N                                     1.595                                                                             "   "          "     "   OMe   Cl     CH                                    1.596                                                                             "   "          "     "   Me    Me     CH                                    1.597                                                                             "   "          "     "   SMe   NEt.sub.2                                                                             N                                     1.598                                                                             "   "          CO.sub.2 -i-Pr                                                                       Me  OMe   Me     N                                     1.599                                                                             "   "          "     "   OMe   OMe    CH                                    1.600                                                                             Me  "          CO.sub.2 -Allyl                                                                      H   OMe   OMe    CH                                    1.601                                                                             Et  "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.602                                                                             "   "          "     H   OMe   Me     N                                     1.603                                                                             "   "          "     "   Me    Me     CH                                    1.604                                                                             "   "          "     "   Cl    OMe    CH                                    1.605                                                                             "   "          "     Me  OMe   OMe    CH                                    1.606                                                                             "   "          "     "   OMe   Me     N                                     1.607                                                                             "   "          CO.sub.2 Et                                                                          H   OMe   OMe    CH                                    1.608                                                                             "   "          "     "   OMe   Me     CH                                    1.609                                                                             "   "          "     "   Cl    OMe    CH                                    1.610                                                                             "   "          "     "   OMe   Me     N                                     1.611                                                                             "   "          "     Me  OMe   OMe    CH                                    1.612                                                                             "   "          "     "   "     Me     N                                     1.613                                                                             "   "          CO.sub.2 -n-Pr                                                                       H   OMe   OMe    CH                                    1.614                                                                             "   "          "     "   OMS   Me     N                                     1.615                                                                             "   "          "     "   OMe   Cl     CH                                    1.616                                                                             "   "          "     "   Me    Me     CH                                    1.617                                                                             "   "          "     Me  OMe   OMe    CH                                    1.618                                                                             "   "          "     "   OMe   Me     N                                     1.619                                                                             "   "          CO.sub.2 -i-Pr                                                                       H   OMe   OMe    CH                                    1.620                                                                             "   "          "     "   OMe   Me     N                                     1.621                                                                             "   "          "     "   Me    Me     CH                                    1.622                                                                             "   "          "     Me  OMe   Me     N                                     1.623                                                                             n-Pr                                                                               CONHEt     CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.624                                                                             "   "          "     "   "     Cl     CH                                    1.625                                                                             "   "          "     "   Me    Me     CH                                    1.626                                                                             "   "          "     "   OMe   Me     N                                     1.627                                                                             "   "          "     Me  OMe   OMe    CH                                    1.628                                                                             "   "          "     "   OMe   Me     N                                     1.629                                                                             n-Pr                                                                               "          CO.sub.2 Et                                                                          H   "     "      N                                     1.630                                                                             "   "          "     "   "     OMe    CH                                    1.631                                                                             "   "          "     "   Me    Me     CH                                    1.632                                                                             "   "          CO.sub.2 -n-Pr                                                                       "   OMe   OMe    CH                                    1.633                                                                             i-Pr                                                                               "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.634                                                                             "   "          "     "   OMe   Me     N                                     1.635                                                                             "   "          "     "   Me    Me     CH                                    1.636                                                                             "   "          "     "   Cl    OMe    N                                     1.637                                                                             "   "          "     Me  OMe   Me     N                                     1.638                                                                             "   "          "     "   "     OMe    CH                                    1.639                                                                             Allyl                                                                              "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.640                                                                             "   "          "     "   "     Cl     CH                                    1.641                                                                             "   "          "     "   Me    Me     CH                                    1.642                                                                             "   "          "     "   OMe   Me     N                                     1.643                                                                             "   "          CO.sub.2 Et                                                                          H   OMe   OMe    CH                                    1.644                                                                             "   "          CO.sub.2 -n-Pr                                                                       "   "     "      CH                                    1.645                                                                             "   "          CO.sub.2 -i-Pr                                                                       "   "     "      CH                                    1.646                                                                             Me  CONHPr     CO.sub.2 Me                                                                          H   "     "      CH                                    1.647                                                                             "   "          "     "   "     OMe    N                                     1.648                                                                             "   "          "     "   "     Me     N                                     1.649                                                                             "   "          "     "   "     "      CH                                    1.650                                                                             "   "          "     "   NMe.sub.2                                                                            OCH.sub.2 CF.sub.3                                                                    N                                     1.651                                                                             "   "          "     "   Me    Me     CH                                    1.652                                                                             "   "          "     "   "     "      N                                     1.653                                                                             "   "          "     "   Cl    OMS    CH                                    1.654                                                                             "   "          "     Me  OMe   OMe    CH                                    1.655                                                                             "   "          "     "   "     Me     N                                     1.656                                                                             "   "          CO.sub.2 Et                                                                          H   OMe   OMe    CH                                    1.657                                                                             "   "          "     "   "     Cl     CH                                    1.658                                                                             "   "          "     "   Me    Me     CH                                    1.659                                                                             "   "          "     "   OMe   Me     N                                     1.660                                                                             "   "          "     "   NMe.sub.2                                                                            OCH.sub.2 CF.sub.3                                                                    N                                     1.661                                                                             "   "          "     Me  OMe   OMe    CH                                    1.662                                                                             "   "          "     "   OMe   Me     N                                     1.663                                                                             "   "          CO.sub.2 -n-Pr                                                                       H   OMe   OMe    CH                                    1.664                                                                             "   "          "     "   "     "      N                                     1.665                                                                             "   "          "     "   OMe   Me     N                                     1.666                                                                             "   "          "     "   Me    Me     CH                                    1.667                                                                             "   "          "     "   OMe   Cl     CH                                    1.668                                                                             "   "          "     Me  Me    OMe    N                                     1.669                                                                             "   "          "     "   OMe   OMe    CH                                    1.670                                                                             Me  CONHPR     CO.sub.2 -i-Pr                                                                       H   OMe   OMe    CH                                    1.671                                                                             "   "          "     "   "     "      N                                     1.672                                                                             "   "          "     "   OMe   Me     N                                     1.673                                                                             "   "          "     "   OMe   Cl     CH                                    1.674                                                                             "   "          "     "   Me    Me     CH                                    1.675                                                                             "   "          "     "   SMe   NEt.sub.2                                                                             N                                     1.676                                                                             "   "          CO.sub.2 -i-Pr                                                                       Me  OMe   Me     N                                     1.677                                                                             "   "          "     "   OMB   OMe    CH                                    1.678                                                                             Me  "          CO.sub.2 -Allyl                                                                      H   OMe   OMe    CH                                    1.679                                                                             Et  "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.680                                                                             "   "          "     H   OMe   Me     N                                     1.681                                                                             "   "          "     "   Me    Me     CH                                    1.682                                                                             "   "          "     "   Cl    OMe    CH                                    1.683                                                                             "   "          "     Me  OMe   OMe    CH                                    1.684                                                                             "   "          "     "   OMe   Me     N                                     1.685                                                                             "   "          CO.sub.2 Et                                                                          H   OMe   OMe    CH                                    1.686                                                                             "   "          "     "   OMe   Me     CH                                    1.687                                                                             "   "          "     "   Cl    OMe    CH                                    1.688                                                                             "   "          "     "   OMe   Me     N                                     1.689                                                                             "   "          "     Me  OMe   OMe    CH                                    1.690                                                                             "   "          "     "   "     Me     N                                     1.691                                                                             "   "          CO.sub.2 -n-Pr                                                                       H   OMe   OMe    CH                                    1.692                                                                             "   "          "     "   OMe   Me     N                                     1.693                                                                             "   "          "     "   OMe   Cl     CH                                    1.694                                                                             "   "          "     "   Me    Me     CH                                    1.695                                                                             "   "          "     Me  OMe   OMe    CH                                    1.696                                                                             "   "          "     "   OMe   Me     N                                     1.697                                                                             "   "          CO.sub.2 -i-Pr                                                                       H   OMe   OMe    CH                                    1.698                                                                             "   "          "     "   OMe   Me     N                                     1.699                                                                             "   "          "     "   Me    Me     CH                                    1.700                                                                             "   "          "     Me  OMe   Me     N                                     1.701                                                                             n-Pr                                                                               "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.702                                                                             "   "          "     "   "     Cl     CH                                    1.703                                                                             "   "          "     "   Me    Me     CH                                    1.704                                                                             "   "          "     "   OMe   Me     N                                     1.705                                                                             "   "          "     Me  OMe   OMe    CH                                    1.706                                                                             "   "          "     "   OMe   Me     N                                     1.707                                                                             n-Pr                                                                               "          CO.sub.2 Et                                                                          H   "     "      N                                     1.708                                                                             "   "          "     "   "     OMe    CH                                    1.709                                                                             "   "          "     "   Me    Me     CH                                    1.710                                                                             "   "          CO.sub.2 -n-Pr                                                                       "   OMe   OMe    CH                                    1.711                                                                             i-Pr                                                                               "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.712                                                                             "   "          "     "   OMe   Me     N                                     1.713                                                                             "   "          "     "   Me    Me     CH                                    1.714                                                                             "   "          "     "   Cl    OMe    N                                     1.715                                                                             "   "          "     Me  OMe   Me     N                                     1.716                                                                             "   "          "     "   "     OMe    CH                                    1.717                                                                             Allyl                                                                              "          CO.sub.2 Me                                                                          H   OMe   OMe    CH                                    1.718                                                                             "   "          "     "   "     Cl     CH                                    1.719                                                                             "   "          "     "   Me    Me     CH                                    1.720                                                                             "   "          "     "   OMe   Me     N                                     1.721                                                                             "   "          CO.sub.2 Et                                                                          H   OMe   OMe    CH                                    __________________________________________________________________________

    __________________________________________________________________________     No. R.sup.1                                                                            R.sup.2   R.sup.3    R.sup.4                                                                            X    Y      Z   m.p.                          __________________________________________________________________________     1.722                                                                              "   "         CO.sub.2 -n-Pr                                                                            "   "    "      CH                                1.723                                                                              "   "         CO.sub.2 -i-Pr                                                                            "   "    "      CH                                1.724                                                                              Me  CONH-allyl                                                                               CO.sub.2Me H   OMe  OMe    CH                                1.725                                                                              "   "         "          "   "    OMe    N                                 1.726                                                                              "   "         "          "   "    Me     N                                 1.727                                                                              "   "         "          "   "    "      CH                                1.728                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 1.729                                                                              "   "         "          "   Me   Me     CH                                1.730                                                                              "   "         "          "   "    "      N                                 1.731                                                                              "   "         "          "   Cl   OMe    CH                                1.732                                                                              "   "         "          Me  OMe  OMe    CH                                1.733                                                                              "   "         "          "   "    Me     N                                 1.734                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                1.735                                                                              "   "         "          "   "    Cl     CH                                1.736                                                                              "   "         "          "   Me   Me     CH                                1.737                                                                              "   "         "          "   OMe  Me     N                                 1.738                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 1.739                                                                              "   "         "          Me  OMe  OMe    CH                                1.740                                                                              "   "         "          "   OMe  Me     N                                 1.741                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                1.742                                                                              "   "         "          "   "    "      N                                 1.743                                                                              "   "         "          "   OMe  Me     N                                 1.744                                                                              "   "         "          "   Me   Me     CH                                1.745                                                                              "   "         "          "   OMe  Cl     CH                                1.746                                                                              "   "         "          Me  Me   OMe    N                                 1.747                                                                              "   "         "          "   OMe  OMe    CH                                1.748                                                                              Me  CONH-allyl                                                                               CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                1.749                                                                              "   "         "          "   "    "      N                                 1.750                                                                              "   "         "          "   OMe  Me     N                                 1.751                                                                              "   "         "          "   OMe  Cl     CH                                1.752                                                                              "   "         "          "   Me   Me     CH                                1.753                                                                              "   "         "          "   SMe  NEt.sub.2                                                                             N                                 1.754                                                                              "   "         CO.sub.2 -i-Pr                                                                            Me  OMe  Me     N                                 1.755                                                                              "   "         "          "   OMe  OMe    CH                                1.756                                                                              Me  "         CO.sub.2 -Allyl                                                                           H   OMe  OMe    CH                                1.757                                                                              Et  "         CO.sub.2Me H   OMe  OMe    CH                                1.758                                                                              "   "         "          H   OMe  Me     N                                 1.759                                                                              "   "         "          "   Me   Me     CH                                1.760                                                                              "   "         "          "   Cl   OMe    CH                                1.761                                                                              "   "         "          Me  OMe  OMe    CH                                1.762                                                                              "   "         "          "   OMe  Me     N                                 1.763                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                1.764                                                                              "   "         "          "   OMe  Me     CH                                1.765                                                                              "   "         "          "   Cl   OMe    CH                                1.766                                                                              "   "         "          "   OMe  Me     N                                 1.767                                                                              "   "         "          Me  OMe  OMe    CH                                1.768                                                                              "   "         "          "   "    Me     N                                 1.769                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                1.770                                                                              "   "         "          "   OMe  Me     N                                 1.771                                                                              "   "         "          "   OMe  Cl     CH                                1.772                                                                              "   "         "          "   Me   Me     CH                                1.773                                                                              "   "         "          Me  OMe  OMe    CH                                1.774                                                                              "   "         "          "   OMe  Me     N                                 1.775                                                                              "   "         CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                1.776                                                                              "   "         "          "   OMe  Me     N                                 1.777                                                                              "   "         "          "   Me   Me     CH                                1.778                                                                              "   "         "          Me  OMe  Me     N                                 1.779                                                                              n-Pr                                                                               CONH-allyl                                                                               CO.sub.2Me H   OMe  OMe    CH                                1.780                                                                              "   "         "          "   "    Cl     CH                                1.781                                                                              "   "         "          "   Me   Me     CH                                1.782                                                                              "   "         "          "   OMe  Me     N                                 1.783                                                                              "   "         "          Me  OMe  OMe    CH                                1.784                                                                              "   "         "          "   OMe  Me     N                                 1.785                                                                              n-Pr                                                                               "         CO.sub.2Et H   OMe  Me     N                                 1.786                                                                              "   "         "          "   "    OMe    CH                                1.787                                                                              "   "         "          "   Me   Me     CH                                1.788                                                                              "   "         CO.sub.2 -n-Pr                                                                            "   OMe  OMe    CH                                1.789                                                                              i-Pr                                                                               "         CO.sub.2Me H   OMe  OMe    CH                                1.790                                                                              "   "         "          "   OMe  Me     N                                 1.791                                                                              "   "         "          "   Me   Me     CH                                1.792                                                                              "   "         "          "   Cl   OMe    N                                 1.793                                                                              "   "         "          Me  OMe  Me     N                                 1.794                                                                              "   "         "          "   "    OMe    CH                                1.795                                                                              Allyl                                                                              "         CO.sub.2Me H   OMe  OMe    CH                                1.796                                                                              "   "         "          "   "    Cl     CH                                1.797                                                                              "   "         "          "   Me   Me     CH                                1.798                                                                              "   "         "          "   OMe  Me     N                                 1.799                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                1.800                                                                              "   "         CO.sub.2 -n-Pr                                                                            "   "    "      "                                 1.801                                                                              "   "         CO.sub.2 -i-Pr                                                                            "   "    "      "                                 1.802                                                                              Me  CSNHMe    CO.sub.2Me H   OMe  OMe    CH                                1.803                                                                              "   "         "          "   "    OMe    N                                 1.804                                                                              "   "         "          "   "    Me     N                                 1.805                                                                              "   "         "          "   "    "      CH                                1.806                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 1.807                                                                              "   "         "          "   Me   Me     CH                                1.808                                                                              "   "         "          "   "    "      N                                 1.809                                                                              "   "         "          "   Cl   OMe    CH                                1.810                                                                              "   "         "          Me  OMe  OMe    CH                                1.811                                                                              "   "         "          "   "    Me     N                                 1.812                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                1.813                                                                              "   "         "          "   "    Cl     CH                                1.814                                                                              "   "         "          "   Me   Me     CH                                1.815                                                                              "   "         "          "   OMe  Me     N                                 1.816                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 1.817                                                                              "   "         "          Me  OMe  OMe    CH                                1.818                                                                              "   "         "          "   OMe  Me     N                                 1.819                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                1.820                                                                              "   "         "          "   "    "      N                                 1.821                                                                              "   "         "          "   OMe  Me     N                                 1.822                                                                              "   "         "          "   Me   Me     CH                                1.823                                                                              "   "         "          "   OMe  Cl     CH                                1.824                                                                              "   "         "          Me  Me   OMe    N                                 1.825                                                                              "   "         "          "   OMe  OMe    CH                                1.826                                                                              Me  CSNHMe    CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                1.827                                                                              "   "         "          "   "    "      N                                 1.828                                                                              "   "         "          "   OMe  Me     N                                 1.829                                                                              "   "         "          "   OMe  Cl     CH                                1.830                                                                              "   "         "          "   Me   Me     CH                                1.831                                                                              "   "         "          "   SMe  NEt.sub.2                                                                             N                                 1.832                                                                              "   "         CO.sub.2 -i-Pr                                                                            Me  OMe  Me     N                                 1.833                                                                              "   "         "          "   OMe  OMe    CH                                1.834                                                                              Me  "         CO.sub.2 -Allyl                                                                           H   OMe  OMe    CH                                1.835                                                                              Et  "         CO.sub.2Me H   OMe  OMe    CH                                1.836                                                                              "   "         "          H   OMe  Me     N                                 1.837                                                                              "   "         "          "   Me   Me     CH                                1.838                                                                              "   "         "          "   Cl   OMe    CH                                1.839                                                                              "   "         "          Me  OMe  OMe    CH                                1.840                                                                              "   "         "          "   OMe  Me     N                                 1.841                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                1.842                                                                              "   "         "          "   OMe  Me     CH                                1.843                                                                              "   "         "          "   Cl   OMe    CH                                1.844                                                                              "   "         "          "   OMe  Me     N                                 1.845                                                                              "   "         "          Me  OMe  OMe    CH                                1.846                                                                              "   "         "          "   "    Me     N                                 1.847                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                1.848                                                                              "   "         "          "   OMe  Me     N                                 1.849                                                                              "   "         "          "   OMe  Cl     CH                                1.850                                                                              "   "         "          "   Me   Me     CH                                1.851                                                                              "   "         "          Me  OMe  OMe    CH                                1.852                                                                              "   "         "          "   OMe  Me     N                                 1.853                                                                              "   "         CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                1.854                                                                              "   "         "          "   OMe  Me     N                                 1.855                                                                              "   "         "          "   Me   Me     CH                                1.856                                                                              "   "         "          Me  OMe  Me     N                                 1.857                                                                              n-Pr                                                                               CSNHMe    CO.sub.2Me H   OMe  OMe    CH                                1.858                                                                              "   "         "          "   "    Cl     CH                                1.859                                                                              "   "         "          "   Me   Me     CH                                1.860                                                                              "   "         "          "   OMe  Me     N                                 1.861                                                                              "   "         "          Me  OMe  OMe    CH                                1.862                                                                              "   "         "          "   OMe  Me     N                                 1.863                                                                              n-Pr                                                                               "         CO.sub.2Et H   "    "      N                                 1.864                                                                              "   "         "          "   "    OMe    CH                                1.865                                                                              "   "         "          "   Me   Me     CH                                1.866                                                                              "   "         CO.sub.2 -n-Pr                                                                            "   OMe  OMe    CH                                1.867                                                                              i-Pr                                                                               "         CO.sub.2Me H   OMe  OMe    CH                                1.868                                                                              "   "         "          "   OMe  Me     N                                 1.869                                                                              "   "         "          "   Me   Me     CH                                1.870                                                                              "   "         "          "   Cl   OMe    N                                 1.871                                                                              "   "         "          Me  OMe  Me     N                                 1.872                                                                              "   "         "          "   "    OMe    CH                                1.873                                                                              Allyl                                                                              "         CO.sub.2Me H   OMe  OMe    CH                                1.874                                                                              "   "         "          "   "    Cl     CH                                1.875                                                                              "   "         "          "   Me   Me     CH                                1.876                                                                              "   "         "          "   OMe  Me     N                                 1.877                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                1.878                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                1.879                                                                              "   "         CO.sub.2 -i-Pr                                                                            "   "    "      "                                 1.880                                                                              Me  CSNHEt    CO.sub.2Me H   OMe  OMe    CH                                1.881                                                                              "   "         "          "   "    OMe    N                                 1.882                                                                              "   "         "          "   "    Me     N                                 1.883                                                                              "   "         "          "   "    "      CH                                1.884                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 1.885                                                                              "   "         "          "   Me   Me     CH                                1.886                                                                              "   "         "          "   "    "      N                                 1.887                                                                              "   "         "          "   Cl   OMe    CH                                1.888                                                                              "   "         "          Me  OMe  OMe    CH                                1.889                                                                              "   "         "          "   "    Me     N                                 1.890                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                1.891                                                                              "   "         "          "   "    Cl     CH                                1.892                                                                              "   "         "          "   Me   Me     CH                                1.893                                                                              "   "         "          "   OMe  Me     N                                 1.894                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 1.895                                                                              "   "         "          Me  OMe  OMe    CH                                1.896                                                                              "   "         "          "   OMe  Me     N                                 1.897                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                1.898                                                                              "   "         "          "   "    "      N                                 1.899                                                                              "   "         "          "   OMe  Me     N                                 1.900                                                                              "   "         "          "   Me   Me     CH                                1.901                                                                              "   "         "          "   OMe  Cl     CH                                1.902                                                                              "   "         "          Me  Me   OMe    N                                 1.903                                                                              "   "         "          "   OMe  OMe    CH                                1.904                                                                              Me  CSNHEt    CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                1.905                                                                              "   "         "          "   "    "      N                                 1.906                                                                              "   "         "          "   OMe  Me     N                                 1.907                                                                              "   "         "          "   OMe  Cl     CH                                1.908                                                                              "   "         "          "   Me   Me     CH                                1.909                                                                              "   "         "          "   SMe  NEt.sub.2                                                                             N                                 1.910                                                                              "   "         CO.sub.2 -i-Pr                                                                            Me  OMe  Me     N                                 1.911                                                                              "   "         "          "   OMe  OMe    CH                                1.912                                                                              Me  "         CO.sub.2 -Allyl                                                                           H   OMe  OMe    CH                                1.913                                                                              Et  "         CO.sub.2Me H   OMe  OMe    CH                                1.914                                                                              "   "         "          H   OMe  Me     N                                 1.915                                                                              "   "         "          "   Me   Me     CH                                1.916                                                                              "   "         "          "   Cl   OMe    CH                                1.917                                                                              "   "         "          Me  OMe  OMe    CH                                1.918                                                                              "   "         "          "   OMe  Me     N                                 1.919                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                1.920                                                                              "   "         "          "   "    Me     CH                                1.921                                                                              "   "         "          "   Cl   OMe    CH                                1.922                                                                              "   "         "          "   OMe  Me     N                                 1.923                                                                              "   "         "          Me  OMe  OMe    CH                                1.924                                                                              "   "         "          "   "    Me     N                                 1.925                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                1.926                                                                              "   "         "          "   OMe  Me     N                                 1.927                                                                              "   "         "          "   OMe  Cl     CH                                1.928                                                                              "   "         "          "   Me   Me     CH                                1.929                                                                              "   "         "          Me  OMe  OMe    CH                                1.930                                                                              "   "         "          "   OMe  Me     N                                 1.931                                                                              "   "         CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                1.932                                                                              "   "         "          "   OMe  Me     N                                 1.933                                                                              "   "         "          "   Me   Me     CH                                1.934                                                                              "   "         "          Me  OMe  Me     N                                 1.935                                                                              n-Pr                                                                               CSNHEt    CO.sub.2Me H   OMe  OMe    CH                                1.936                                                                              "   "         "          "   "    Cl     CH                                1.937                                                                              "   "         "          "   Me   Me     CH                                1.938                                                                              "   "         "          "   OMe  Me     N                                 1.939                                                                              "   "         "          Me  OMe  OMe    CH                                1.940                                                                              "   "         "          "   OMe  Me     N                                 1.941                                                                              n-Pr                                                                               "         CO.sub.2Et H   "    "      N                                 1.942                                                                              "   "         "          "   "    OMe    CH                                1.943                                                                              "   "         "          "   Me   Me     CH                                1.944                                                                              "   "         CO.sub.2 -n-Pr                                                                            "   OMe  OMe    CH                                1.945                                                                              i-Pr                                                                               "         CO.sub.2Me H   OMe  OMe    CH                                1.946                                                                              "   "         "          "   OMe  Me     N                                 1.947                                                                              "   "         "          "   Me   Me     CH                                1.948                                                                              "   "         "          "   Cl   OMe    N                                 1.949                                                                              "   "         "          Me  OMe  Me     N                                 1.950                                                                              "   "         "          "   "    OMe    CH                                1.951                                                                              Allyl                                                                              "         CO.sub.2Me H   OMe  OMe    CH                                1.952                                                                              "   "         "          "   "    Cl     CH                                1.953                                                                              "   "         "          "   Me   Me     CH                                1.954                                                                              "   "         "          "   OMe  Me     N                                 1.955                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                1.956                                                                              "   "         CO.sub.2 -n-Pr                                                                            "   "    "      CH                                1.957                                                                              "   "         CO.sub.2 -i-Pr                                                                            "   "    "      CH                                1.958                                                                              Me  CSNH-n-Pr CO.sub.2Me H   OMe  OMe    CH                                1.959                                                                              "   "         "          "   "    OMe    N                                 1.960                                                                              "   "         "          "   "    Me     N                                 1.961                                                                              "   "         "          "   "    "      CH                                1.962                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 1.963                                                                              "   "         "          "   Me   Me     CH                                1.964                                                                              "   "         "          "   "    "      N                                 1.965                                                                              "   "         "          "   Cl   OMe    CH                                1.966                                                                              "   "         "          Me  OMe  OMe    CH                                1.967                                                                              "   "         "          "   "    Me     N                                 1.968                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                1.969                                                                              "   "         "          "   "    Cl     CH                                1.970                                                                              "   "         "          "   Me   Me     CH                                1.971                                                                              "   "         "          "   OMe  Me     N                                 1.972                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 1.973                                                                              "   "         "          Me  OMe  OMe    CH                                1.974                                                                              "   "         "          "   OMe  Me     N                                 1.975                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                1.976                                                                              "   "         "          "   "    "      N                                 1.977                                                                              "   "         "          "   OMe  Me     N                                 1.978                                                                              "   "         "          "   Me   Me     CH                                1.979                                                                              "   "         "          "   OMe  Cl     CH                                1.980                                                                              "   "         "          Me  Me   OMe    N                                 1.981                                                                              "   "         "          "   OMe  OMe    CH                                1.982                                                                              Me  CSNH-n-Pr CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                1.983                                                                              "   "         "          "   "    "      N                                 1.984                                                                              "   "         "          "   OMe  Me     N                                 1.985                                                                              "   "         "          "   OMe  Cl     CH                                1.986                                                                              "   "         "          "   Me   Me     CH                                1.987                                                                              "   "         "          "   SMe  NEt.sub.2                                                                             N                                 1.988                                                                              "   "         CO.sub.2 -i-Pr                                                                            Me  OMe  Me     N                                 1.989                                                                              "   "         "          "   OMe  OMe    CH                                1.990                                                                              Me  "         CO.sub.2 -Allyl                                                                           H   OMe  OMe    CH                                1.991                                                                              Et  "         CO.sub.2Me H   OMe  OMe    CH                                1.992                                                                              "   "         "          H   OMe  Me     N                                 1.993                                                                              "   "         "          "   Me   Me     CH                                1.994                                                                              "   "         "          "   Cl   OMe    CH                                1.995                                                                              "   "         "          Me  OMe  OMe    CH                                1.996                                                                              "   "         "          "   OMe  Me     N                                 1.997                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                1.998                                                                              "   "         "          "   OMe  Me     CH                                1.999                                                                              "   "         "          "   Cl   OMe    CH                                2.000                                                                              "   "         "          "   OMe  Me     N                                 2.001                                                                              "   "         "          Me  OMe  OMe    CH                                2.002                                                                              "   "         "          "   "    Me     N                                 2.003                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                2.004                                                                              "   "         "          "   OMe  Me     N                                 2.005                                                                              "   "         "          "   OMe  Cl     CH                                2.006                                                                              "   "         "          "   Me   Me     CH                                2.007                                                                              "   "         "          Me  OMe  OMe    CH                                2.008                                                                              "   "         "          "   OMe  Me     N                                 2.009                                                                              "   "         CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                2.010                                                                              "   "         "          "   OMe  Me     N                                 2.011                                                                              "   "         "          "   Me   Me     CH                                2.012                                                                              "   "         "          Me  OMe  Me     N                                 2.013                                                                              n-Pr                                                                               CSNH-n-Pr CO.sub.2Me H   OMe  OMe    CH                                2.014                                                                              "   "         "          "   "    Cl     CH                                2.015                                                                              "   "         "          "   Me   Me     CH                                2.016                                                                              "   "         "          "   OMe  Me     N                                 2.017                                                                              "   "         "          Me  OMe  OMe    CH                                2.018                                                                              "   "         "          "   OMe  Me     N                                 2.019                                                                              n-Pr                                                                               "         CO.sub.2Et H   "    "      N                                 2.020                                                                              "   "         "          "   "    OMe    CH                                2.021                                                                              "   "         "          "   Me   Me     CH                                2.022                                                                              "   "         CO.sub.2 -n-Pr                                                                            "   OMe  OMe    CH                                2.023                                                                              i-Pr                                                                               "         CO.sub.2Me H   "    "      CH                                2.024                                                                              "   "         "          "   "    Me     N                                 2.025                                                                              "   "         "          "   Me   Me     CH                                2.026                                                                              "   "         "          "   Cl   OMe    N                                 2.027                                                                              "   "         "          Me  OMe  Me     N                                 2.028                                                                              "   "         "          "   "    OMe    CH                                2.029                                                                              Allyl                                                                              "         CO.sub.2Me H   OMe  OMe    CH                                2.030                                                                              "   "         "          "   "    Cl     CH                                2.031                                                                              "   "         "          "   Me   Me     CH                                2.032                                                                              "   "         "          "   OMe  Me     N                                 2.033                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                2.034                                                                              "   "         CO.sub.2 -n-Pr                                                                            "   "    "      CH                                2.035                                                                              "   "         CO.sub.2 -i-Pr                                                                            "   "    "      CH                                2.036                                                                              Me  CSNH-i-Pr CO.sub.2Me H   OMe  OMe    CH                                2.037                                                                              "   "         "          "   "    OMe    N                                 2.038                                                                              "   "         "          "   "    Me     N                                 2.039                                                                              "   "         "          "   "    "      CH                                2.040                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 2.041                                                                              "   "         "          "   Me   Me     CH                                2.042                                                                              "   "         "          "   "    "      N                                 2.043                                                                              "   "         "          "   Cl   OMe    CH                                2.044                                                                              "   "         "          Me  OMe  OMe    CH                                2.045                                                                              "   "         "          "   "    Me     N                                 2.046                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                2.047                                                                              "   "         "          "   "    Cl     CH                                2.048                                                                              "   "         "          "   Me   Me     CH                                2.049                                                                              "   "         "          "   OMe  Me     N                                 2.050                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 2.051                                                                              "   "         "          Me  OMe  OMe    CH                                2.052                                                                              "   "         "          "   OMe  Me     N                                 2.053                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                2.054                                                                              "   "         "          "   "    "      N                                 2.055                                                                              "   "         "          "   OMe  Me     N                                 2.056                                                                              "   "         "          "   Me   Me     CH                                2.057                                                                              "   "         "          "   OMe  Cl     CH                                2.058                                                                              "   "         "          Me  Me   OMe    N                                 2.059                                                                              "   "         "          "   OMe  OMe    CH                                2.060                                                                              Me  CSNH-i-Pr CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                2.061                                                                              "   "         "          "   "    "      N                                 2.062                                                                              "   "         "          "   OMe  Me     N                                 2.063                                                                              "   "         "          "   OMe  Cl     CH                                2.064                                                                              "   "         "          "   Me   Me     CH                                2.065                                                                              "   "         "          "   SMe  NEt.sub.2                                                                             N                                 2.066                                                                              "   "         CO.sub.2 -i-Pr                                                                            Me  OMe  Me     N                                 2.067                                                                              "   "         "          "   OMe  OMe    CH                                2.068                                                                              Me  "         CO.sub.2 -Allyl                                                                           H   OMe  OMe    CH                                2.069                                                                              Et  "         CO.sub.2Me H   OMe  OMe    CH                                2.070                                                                              "   "         "          H   OMe  Me     N                                 2.071                                                                              "   "         "          "   Me   Me     CH                                2.072                                                                              "   "         "          "   Cl   OMe    CH                                2.073                                                                              "   "         "          Me  OMe  OMe    CH                                2.074                                                                              "   "         "          "   OMe  Me     N                                 2.075                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                2.076                                                                              "   "         "          "   OMe  Me     CH                                2.077                                                                              "   "         "          "   Cl   OMe    CH                                2.078                                                                              "   "         "          "   OMe  Me     N                                 2.079                                                                              "   "         "          Me  OMe  OMe    CH                                2.080                                                                              "   "         "          "   "    Me     N                                 2.081                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                2.082                                                                              "   "         "          "   OMe  Me     N                                 2.083                                                                              "   "         "          "   OMe  Cl     CH                                2.084                                                                              "   "         "          "   Me   Me     CH                                2.085                                                                              "   "         "          Me  OMe  OMe    CH                                2.086                                                                              "   "         "          "   OMe  Me     N                                 2.087                                                                              "   "         CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                2.088                                                                              "   "         "          "   OMe  Me     N                                 2.089                                                                              "   "         "          "   Me   Me     CH                                2.090                                                                              "   "         "          Me  OMe  Me     N                                 2.091                                                                              n-Pr                                                                               CSNH-i-Pr CO.sub.2Me H   OMe  OMe    CH                                2.092                                                                              "   "         "          "   "    Cl     CH                                2.093                                                                              "   "         "          "   Me   Me     CH                                2.094                                                                              "   "         "          "   OMe  Me     N                                 2.095                                                                              "   "         "          Me  OMe  OMe    CH                                2.096                                                                              "   "         "          "   OMe  Me     N                                 2.097                                                                              n-Pr                                                                               "         CO.sub. 2Et                                                                               H   "    "      N                                 2.098                                                                              "   "         "          "   "    OMe    CH                                2.099                                                                              "   "         "          "   Me   Me     CH                                2.100                                                                              "   "         CO.sub.2 -n-Pr                                                                            "   OMe  OMe    CH                                2.101                                                                              i-Pr                                                                               "         CO.sub.2Me H   OMe  OMe    CH                                2.102                                                                              "   "         "          "   OMe  Me     N                                 2.103                                                                              "   "         "          "   Me   Me     CH                                2.104                                                                              "   "         "          "   Cl   OMe    N                                 2.105                                                                              "   "         "          Me  OMe  Me     N                                 2.106                                                                              "   "         "          "   "    OMe    CH                                2.107                                                                              Allyl                                                                              "         CO.sub.2Me H   OMe  OMe    CH                                2.108                                                                              "   "         "          "   "    Cl     CH                                2.109                                                                              "   "         "          "   Me   Me     CH                                2.110                                                                              "   "         "          "   OMe  Me     N                                 2.111                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                2.112                                                                              "   "         CO.sub.2 -n-Pr                                                                            "   "    "      CH                                2.113                                                                              "   "         CO.sub.2 -i-Pr                                                                            "   "    "      CH                                2.114                                                                              Me  CSNH-allyl                                                                               CO.sub.2Me H   OMe  OMe    CH                                2.115                                                                              "   "         "          "   "    OMe    N                                 2.116                                                                              "   "         "          "   "    Me     N                                 2.117                                                                              "   "         "          "   "    "      CH                                2.118                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 2.119                                                                              "   "         "          "   Me   Me     CH                                2.120                                                                              "   "         "          "   "    "      N                                 2.121                                                                              "   "         "          "   Cl   OMe    CH                                2.122                                                                              "   "         "          Me  OMe  OMe    CH                                2.123                                                                              "   "         "          "   "    Me     N                                 2.124                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                2.125                                                                              "   "         "          "   "    Cl     CH                                2.126                                                                              "   "         "          "   Me   Me     CH                                2.127                                                                              "   "         "          "   OMe  Me     N                                 2.128                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 2.129                                                                              "   "         "          Me  OMe  OMe    CH                                2.130                                                                              "   "         "          "   OMe  Me     N                                 2.131                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                2.132                                                                              "   "         "          "   "    "      N                                 2.133                                                                              "   "         "          "   OMe  Me     N                                 2.134                                                                              "   "         "          "   Me   Me     CH                                2.135                                                                              "   "         "          "   OMe  Cl     CH                                2.136                                                                              "   "         "          Me  Me   OMe    N                                 2.137                                                                              "   "         "          "   OMe  OMe    CH                                2.138                                                                              Me  CSNH-allyl                                                                               CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                2.139                                                                              "   "         "          "   "    "      N                                 2.140                                                                              "   "         "          "   H    Me     N                                 2.141                                                                              "   "         "          "   OMe  Cl     CH                                2.142                                                                              "   "         "          "   Me   Me     CH                                2.143                                                                              "   "         "          "   SMe  NEt.sub.2                                                                             N                                 2.144                                                                              "   "         CO.sub.2 -i-Pr                                                                            Me  OMe  Me     N                                 2.145                                                                              "   "         "          "   OMe  OMe    CH                                2.146                                                                              Me  "         CO.sub.2 -Allyl                                                                           H   OMe  OMe    CH                                2.147                                                                              Et  "         CO.sub.2Me H   OMe  OMe    CH                                2.148                                                                              "   "         "          H   OMe  Me     N                                 2.149                                                                              "   "         "          "   Me   Me     CH                                2.150                                                                              "   "         "          "   Cl   OMe    CH                                2.151                                                                              "   "         "          Me  OMe  OMe    CH                                2.152                                                                              "   "         "          "   OMe  Me     N                                 2.153                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                2.154                                                                              "   "         "          "   OMe  Me     CH                                2.155                                                                              "   "         "          "   Cl   OMe    CH                                2.156                                                                              "   "         "          "   OMe  Me     N                                 2.157                                                                              "   "         "          Me  OMe  OMe    CH                                2.158                                                                              "   "         "          "   "    Me     N                                 2.159                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                2.160                                                                              "   "         "          "   OMe  Me     N                                 2.161                                                                              "   "         "          "   OMe  Cl     CH                                2.162                                                                              "   "         "          "   Me   Me     CH                                2.163                                                                              "   "         "          Me  OMe  OMe    CH                                2.164                                                                              "   "         "          "   OMe  Me     N                                 2.165                                                                              "   "         CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                2.166                                                                              "   "         "          "   OMe  Me     N                                 2.167                                                                              "   "         "          "   Me   Me     CH                                2.168                                                                              "   "         "          Me  OMe  Me     N                                 2.169                                                                              n-Pr                                                                               CSNH-allyl                                                                               CO.sub.2Me H   OMe  OMe    CH                                2.170                                                                              "   "         "          "   "    Cl     CH                                2.171                                                                              "   "         "          "   Me   Me     CH                                2.172                                                                              "   "         "          "   OMe  Me     N                                 2.173                                                                              "   "         "          Me  OMe  OMe    CH                                2.174                                                                              "   "         "          "   OMe  Me     N                                 2.175                                                                              n-Pr                                                                               "         CO.sub.2Et H   "    "      N                                 2.176                                                                              "   "         "          "   "    OMe    CH                                2.177                                                                              "   "         "          "   Me   Me     CH                                2.178                                                                              "   "         CO.sub.2 -n-Pr                                                                            "   OMe  OMe    CH                                2.179                                                                              i-Pr                                                                               "         CO.sub.2Me H   OMe  OMe    CH                                2.180                                                                              "   "         "          "   OMe  Me     N                                 2.181                                                                              "   "         "          "   Me   Me     CH                                2.182                                                                              "   "         "          "   Cl   OMe    N                                 2.183                                                                              "   "         "          Me  OMe  Me     N                                 2.184                                                                              "   "         "          "   "    OMe    CH                                2.185                                                                              Allyl                                                                              "         CO.sub.2Me H   OMe  OMe    CH                                2.186                                                                              "   "         "          "   "    Cl     CH                                2.187                                                                              "   "         "          "   Me   Me     CH                                2.188                                                                              "   "         "          "   OMe  Me     N                                 2.189                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                2.190                                                                              "   "         CO.sub.2 -n-Pr                                                                            "   "    "      CH                                2.191                                                                              "   "         CO.sub.2 -i-Pr                                                                            "   "    "      CH                                2.192                                                                              Me  CSNHCO.sub.2 Et                                                                          CO.sub.2Me H   OMe  OMe    CH  144-145° C.            2.193                                                                              "   "         "          "   "    OMe    N                                 2.194                                                                              "   "         "          "   "    Me     N                                 2.195                                                                              "   "         "          "   "    "      CH                                2.196                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 2.197                                                                              "   "         "          "   Me   Me     CH                                2.198                                                                              "   "         "          "   "    "      N                                 2.199                                                                              "   "         "          "   Cl   OMe    CH                                2.200                                                                              "   "         "          Me  OMe  OMe    CH                                2.201                                                                              "   "         "          "   "    Me     N                                 2.202                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                2.203                                                                              "   "         "          "   "    Cl     CH                                2.204                                                                              "   "         "          "   Me   Me     CH                                2.205                                                                              "   "         "          "   OMe  Me     N                                 2.206                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 2.207                                                                              "   "         "          M   OMe  OMe    CH                                2.208                                                                              "   "         "          "   OMe  Me     N                                 2.209                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                2.210                                                                              "   "         "          "   "    "      N                                 2.211                                                                              "   "         "          "   OMe  OMe    N                                 2.212                                                                              "   "         "          "   Me   Me     CH                                2.213                                                                              "   "         "          "   OMe  Cl     CH                                2.214                                                                              "   "         "          Me  Me   OMe    N                                 2.215                                                                              "   "         "          "   OMe  OMe    CH                                2.216                                                                              Me  CSNHCO.sub.2 Et                                                                          CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                2.217                                                                              "   "         "          "   "    "      N                                 2.218                                                                              "   "         "          "   OMe  Me     N                                 2.219                                                                              "   "         "          "   OMe  Cl     CH                                2.220                                                                              "   "         "          "   Me   Me     CH                                2.221                                                                              "   "         "          "   SMe  NEt.sub.2                                                                             N                                 2.222                                                                              "   "         CO.sub.2 -i-Pr                                                                            Me  OMe  Me     N                                 2.223                                                                              "   "         "          "   OMe  OMe    CH                                2.224                                                                              Me  "         CO.sub.2 -Allyl                                                                           H   OMe  OMe    CH                                2.225                                                                              Et  "         CO.sub.2Me H   OMe  OMe    CH                                2.226                                                                              "   "         "          H   OMe  Me     N                                 2.227                                                                              "   "         "          "   Me   Me     CH                                2.228                                                                              "   "         "          "   Cl   OMe    CH                                2.229                                                                              "   "         "          Me  OMe  OMe    CH                                2.230                                                                              "   "         "          "   OMe  Me     N                                 2.231                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                2.232                                                                              "   "         "          "   OMe  Me     CH                                2.233                                                                              "   "         "          "   Cl   OMe    CH                                2.234                                                                              "   "         "          "   OMe  Me     N                                 2.235                                                                              "   "         "          Me  OMe  OMe    CH                                2.236                                                                              "   "         "          "   "    Me     N                                 2.237                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                2.238                                                                              "   "         "          "   OMe  Me     N                                 2.239                                                                              "   "         "          "   OMe  Cl     CH                                2.240                                                                              "   "         "          "   Me   Me     CH                                2.241                                                                              "   "         "          Me  OMe  OMe    CH                                2.242                                                                              "   "         "          "   OMe  Me     N                                 2.243                                                                              "   "         CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                2.244                                                                              "   "         "          "   OMe  Me     N                                 2.245                                                                              "   "         "          "   Me   Me     CH                                2.246                                                                              "   "         "          Me  OMe  Me     N                                 2.247                                                                              n-Pr                                                                               CSNHCO.sub.2 Et                                                                          CO.sub.2Me H   OMe  OMe    CH                                2.248                                                                              "   "         "          "   "    Cl     CH                                2.249                                                                              "   "         "          "   Me   Me     CH                                2.250                                                                              "   "         "          "   OMe  Me     N                                 2.251                                                                              "   "         "          Me  OMe  OMe    CH                                2.252                                                                              "   "         "          "   OMe  Me     N                                 2.253                                                                              n-Pr                                                                               "         CO.sub.2Et H   "    "      N                                 2.254                                                                              "   "         "          "   "    OMe    CH                                2.255                                                                              "   "         "          "   Me   Me     CH                                2.256                                                                              "   "         CO.sub.2 -n-Pr                                                                            "   OMe  OMe    CH                                2.257                                                                              i-Pr                                                                               "         CO.sub.2Me H   OMe  OMe    CH                                2.258                                                                              "   "         "          "   OMe  Me     N                                 2.259                                                                              "   "         "          "   Me   Me     CH                                2.260                                                                              "   "         "          "   Cl   OMe    N                                 2.261                                                                              "   "         "          Me  OMe  Me     N                                 2.262                                                                              "   "         "          "   "    OMe    CH                                2.263                                                                              Allyl                                                                              "         CO.sub.2Me H   OMe  OMe    CH                                2.264                                                                              "   "         "          "   "    Cl     CH                                2.265                                                                              "   "         "          "   Me   Me     CH                                2.266                                                                              "   "         "          "   OMe  Me     N                                 2.267                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                2.268                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                2.269                                                                              "   "         CO.sub.2 -i-Pr                                                                            "   "    "      CH                                2.270                                                                              Me  SO.sub.2 NHMe                                                                            CO.sub.2Me H   OMe  OMe    CH  117-118° C.            2.271                                                                              "   "         "          "   "    OMe    N                                 2.272                                                                              "   "         "          "   "    Me     N                                 2.273                                                                              "   "         "          "   "    "      CH                                2.274                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 2.275                                                                              "   "         "          "   Me   Me     CH                                2.276                                                                              "   "         "          "   "    "      N                                 2.277                                                                              "   "         "          "   Cl   OMe    CH                                2.278                                                                              "   "         "          Me  OMe  OMe    CH                                2.279                                                                              "   "         "          "   "    Me     N                                 2.280                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                2.281                                                                              "   "         "          "   "    Cl     CH                                2.282                                                                              "   "         "          "   Me   Me     CH                                2.283                                                                              "   "         "          "   OMe  Me     N                                 2.284                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 2.285                                                                              "   "         "          Me  OMe  OMe    CH                                2.286                                                                              "   "         "          "   OMe  Me     N                                 2.287                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                2.288                                                                              "   "         "          "   "    "      N                                 2.289                                                                              "   "         "          "   OMe  Me     N                                 2.290                                                                              "   "         "          "   Me   Me     CH                                2.291                                                                              "   "         "          "   OMe  Cl     CH                                2.292                                                                              "   "         "          Me  Me   OMe    N                                 2.293                                                                              "   "         "          "   OMe  OMe    CH                                2.294                                                                              Me  SO.sub.2NHMe                                                                             CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                2.295                                                                              "   "         "          "   "    "      N                                 2.296                                                                              "   "         "          "   OMe  Me     N                                 2.297                                                                              "   "         "          "   Me   Me     CH                                2.298                                                                              "   "         "          "   Me   Me     CH                                2.299                                                                              "   "         "          "   SMe  NEt.sub.2                                                                             N                                 2.300                                                                              "   "         CO.sub.2 -i-Pr                                                                            Me  OMe  Me     N                                 2.301                                                                              "   "         "          "   OMe  OMe    CH                                2.302                                                                              Me  "         CO.sub.2 -Allyl                                                                           H   OMe  OMe    CH                                2.303                                                                              Et  "         CO.sub.2Me H   OMe  OMe    CH                                2.304                                                                              "   "         "          H   OMe  Me     N                                 2.305                                                                              "   "         "          "   Me   Me     CH                                2.306                                                                              "   "         "          "   Cl   OMe    CH                                2.307                                                                              "   "         "          Me  OMe  OMe    CH                                2.308                                                                              "   "         "          "   OMe  Me     N                                 2.309                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                2.310                                                                              "   "         "          "   OMe  Me     CH                                2.311                                                                              "   "         "          "   Cl   OMe    CH                                2.312                                                                              "   "         "          "   OMe  Me     N                                 2.313                                                                              "   "         "          Me  OMe  OMe    CH                                2.314                                                                              "   "         "          "   "    Me     N                                 2.315                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                2.316                                                                              "   "         "          "   OMe  Me     N                                 2.317                                                                              "   "         "          "   OMe  Cl     CH                                2.318                                                                              "   "         "          "   Me   Me     CH                                2.319                                                                              "   "         "          Me  OMe  OMe    CH                                2.320                                                                              "   "         "          "   OMe  Me     N                                 2.321                                                                              "   "         CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                2.322                                                                              "   "         "          "   OMe  Me     N                                 2.323                                                                              "   "         "          "   Me   Me     CH                                2.324                                                                              "   "         "          Me  OMe  Me     N                                 2.325                                                                              n-Pr                                                                               SO.sub.2 NHMe                                                                            CO.sub.2Me H   OMe  OMe    CH                                2.326                                                                              "   "         "          "   "    Cl     CH                                2.327                                                                              "   "         "          "   Me   Me     CH                                2.328                                                                              "   "         "          "   OMe  Me     N                                 2.329                                                                              "   "         "          Me  OMe  OMe    CH                                2.330                                                                              "   "         "              OMe  Me     N                                 2.331                                                                              n-Pr                                                                               "         CO.sub.2Et H   "    "      N                                 2.332                                                                              "   "         "          "   "    OMe    CH                                2.333                                                                              "   "         "          "   Me   Me     CH                                2.334                                                                              "   "         CO.sub.2 -n-Pr                                                                            "   OMe  OMe    CH                                2.335                                                                              i-Pr                                                                               "         CO.sub.2Me H   OMe  OMe    CH                                2.336                                                                              "   "         "          "   OMe  Me     N                                 2.337                                                                              "   "         "          "   Me   Me     CH                                2.338                                                                              "   "         "          "   Cl   OMe    N                                 2.339                                                                              "   "         "          Me  OMe  Me     N                                 2.340                                                                              "   "         "          "   "    OMe    CH                                2.341                                                                              Allyl                                                                              "         CO.sub.2Me H   OMe  OMe    CH                                2.342                                                                              "   "         "          "   "    Cl     CH                                2.343                                                                              "   "         "          "   Me   Me     CH                                2.344                                                                              "   "         "          "   OMe  Me     N                                 2.345                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                2.346                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                2.347                                                                              "   "         CO.sub.2 -i-Pr                                                                            "   "    "      CH                                2.348                                                                              Me  SO.sub.2 NMe.sub.2                                                                       CO.sub.2Me H   OMe  OMe    CH                                2.349                                                                              "   "         "          "   "    OMe    N                                 2.350                                                                              "   "         "          "   "    Me     N                                 2.351                                                                              "   "         "          "   "    "      CH                                2.352                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 2.353                                                                              "   "         "          "   Me   Me     CH                                2.354                                                                              "   "         "          "   "    "      N                                 2.355                                                                              "   "         "          "   Cl   OMe    CH                                2.356                                                                              "   "         "          Me  OMe  OMe    CH                                2.357                                                                              "   "         "          "   "    Me     N                                 2.358                                                                              "   "         CO.sub.2 Et                                                                               H   OMe  OMe    CH                                2.359                                                                              "   "         "          "   "    Cl     CH                                2.360                                                                              "   "         "          "   Me   Me     CH                                2.361                                                                              "   "         "          "   OMe  Me     N                                 2.362                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 2.363                                                                              "   "         "          Me  OMe  OMe    CH                                2.364                                                                              "   "         "          "   OMe  Me     N                                 2.365                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                2.366                                                                              "   "         "          "   "    "      N                                 2.367                                                                              "   "         "          "   OMe  Me     N                                 2.368                                                                              "   "         "          "   Me   Me     CH                                2.369                                                                              "   "         "          "   OMe  Cl     CH                                2.370                                                                              "   "         "          Me  Me   OMe    N                                 2.371                                                                              "   "         "          "   OMe  OMe    CH                                2.372                                                                              Me  SO.sub.2 NMe.sub.2                                                                       CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                2.373                                                                              "   "         "          "   "    "      N                                 2.374                                                                              "   "         "          "   OMe  Me     N                                 2.375                                                                              "   "         "          "   OMe  Cl     CH                                2.376                                                                              "   "         "          "   Me   Me     CH                                2.377                                                                              "   "         "          "   SMe  NEt.sub.2                                                                             N                                 2.378                                                                              "   "         CO.sub.2 -i-Pr                                                                            Me  OMe  Me     N                                 2.379                                                                              "   "         "          "   OMe  OMe    CH                                2.380                                                                              Me  "         CO.sub.2 -Allyl                                                                           H   OMe  OMe    CH                                2.381                                                                              Et  "         CO.sub.2Me H   OMe  OMe    CH                                2.382                                                                              "   "         "          H   OMe  Me     N                                 2.383                                                                              "   "         "          "   Me   Me     CH                                2.384                                                                              "   "         "          "   Cl   OMe    CH                                2.385                                                                              "   "         "          Me  OMe  OMe    CH                                2.386                                                                              "   "         "          "   OMe  Me     N                                 2.387                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                2.388                                                                              "   "         "          "   OMe  Me     CH                                2.389                                                                              "   "         "          "   Cl   OMe    CH                                2.390                                                                              "   "         "          "   OMe  Me     N                                 2.391                                                                              "   "         "          Me  OMe  OMe    CH                                2.392                                                                              "   "         "          "   "    Me     N                                 2.393                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                2.394                                                                              "   "         "          "   OMe  Me     N                                 2.395                                                                              "   "         "          "   OMe  Cl     CH                                2.396                                                                              "   "         "          "   Me   Me     CH                                2.397                                                                              "   "         "          Me  OMe  OMe    CH                                2.398                                                                              "   "         "          "   OMe  Me     N                                 2.399                                                                              "   "         CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                2.400                                                                              "   "         "          "   OMe  Me     N                                 2.401                                                                              "   "         "          "   Me   Me     CH                                2.402                                                                              "   "         "          Me  OMe  Me     N                                 2.403                                                                              n-Pr                                                                               SO.sub.2 NMe.sub.2                                                                       CO.sub.2Me H   OMe  OMe    CH                                2.404                                                                              "   "         "          "   "    Cl     CH                                2.405                                                                              "   "         "          "   Me   Me     CH                                2.406                                                                              "   "         "          "   OMe  Me     N                                 2.407                                                                              "   "         "          Me  OMe  OMe    CH                                2.408                                                                              "   "         "          "   OMe  Me     N                                 2.409                                                                              n-Pr                                                                               "         CO.sub.2Et H   OMe  Me     N                                 2.410                                                                              "   "         "          "   "    OMe    CH                                2.411                                                                              "   "         "          "   Me   Me     CH                                2.412                                                                              "   "         CO.sub.2 -n-Pr                                                                            "   OMe  OMe    CH                                2.413                                                                              i-Pr                                                                               "         CO.sub.2Me H   OMe  OMe    CH                                2.414                                                                              "   "         "          "   OMe  Me     N                                 2.415                                                                              "   "         "          "   Me   Me     CH                                2.416                                                                              "   "         "          "   Cl   OMe    N                                 2.417                                                                              "   "         "          Me  OMe  Me     N                                 2.418                                                                              "   "         "          "   "    OMe    CH                                2.419                                                                              Allyl                                                                              "         CO.sub.2Me H   OMe  OMe    CH                                2.420                                                                              "   "         "          "   "    Cl     CH                                2.421                                                                              "   "         "          "   Me   Me     CH                                2.422                                                                              "   "         "          "   OMe  Me     N                                 2.423                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                2.424                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                2.425                                                                              "   "         CO.sub.2 -i-Pr                                                                            "   "    "      CH                                2.426                                                                              Me  CHO                                                                                       ##STR22## H   OMe  OMe    CH                                2.427                                                                              "   "         "          H   OMe  Me     N                                 2.428                                                                              "   "         "          "   Me   Me     CH                                2.429                                                                              "   COCH.sub.3                                                                               "          "   OMe  OMe    CH                                2.430                                                                              "   "         "          "   OMe  Me     N                                 2.431                                                                              "   "         "          "   Me   Me     CH                                2.432                                                                              "   COCH.sub.2 CH.sub.3                                                                      "          "   OMe  OMe    CH                                2.433                                                                              Et  CHO       "          "   "    "      CH                                2.434                                                                              Pr  "         "          "   "    "      CH                                2.435                                                                              Et  COCH.sub.3                                                                               "          "   "    "      CH                                2.436                                                                              Pr  "         "          "   "    "      CH                                2.437                                                                              Et  COCH.sub.2 CH.sub.3                                                                      "          "   "    "      CH                                2.438                                                                              Me                                                                                  ##STR23##                                                                               "          "   "    "      CH                                2.439                                                                              Me  CO.sub.2 Me                                                                              "          "   "    "      CH                                2.440                                                                              Et  "         "          "   "    "      CH                                2.441                                                                              Pr  "         "          "   "    "      CH                                2.442                                                                              Me  CONHEt    "          "   "    "      CH                                2.443                                                                              Et  "         "          "   "    "      CH                                2.444                                                                              Pr  "         "          "   "    "      CH                                2.445                                                                              Me  CHO                                                                                       ##STR24## H   OMe  OMe    CH                                2.446                                                                              "   "         "          H   OMe  Me     N                                 2.447                                                                              "   "         "          "   Me   Me     CH                                2.448                                                                              "   COCH.sub.3                                                                               "          "   OMe  OMe    CH                                2.449                                                                              "   "         "          "   OMe  Me     N                                 2.450                                                                              "   "         "          "   Me   Me     CH                                2.451                                                                              "   COCH.sub.2 CH.sub.3                                                                      "          "   OMe  OMe    CH                                2.452                                                                              Et  CHO       "          "   "    "      CH                                2.453                                                                              Pr  "         "          "   "    "      CH                                2.454                                                                              Et  COCH.sub.3                                                                               "          "   "    "      CH                                2.455                                                                              Pr  "         "          "   "    "      CH                                2.456                                                                              Et  COCH.sub.2 CH.sub. 3                                                                     "          "   "    "      CH                                2.457                                                                              Me                                                                                  ##STR25##                                                                               "          "   "    "      CH                                2.458                                                                              Me  CO.sub.2 Me                                                                              "          "   "    "      CH                                2.459                                                                              Et  "         "          "   "    "      CH                                2.460                                                                              Pr  "         "          "   "    "      CH                                2.461                                                                              Me  CONHEt    "          "   "    "      CH                                2.462                                                                              Et  "         "          "   "    "      CH                                2.463                                                                              Pr  "         "          "   "    "      CH                                2.464                                                                              Me  CHO       CO.sub.2NCHMe.sub.2                                                                       H   OMe  OMe    CH                                2.465                                                                              "   "         "          H   OMe  Me     N                                 2.466                                                                              "   "         "          "   Me   Me     CH                                2.467                                                                              "   COCH.sub.3                                                                               "          "   OMe  OMe    CH                                2.468                                                                              "   "         "          "   OMe  Me     N                                 2.469                                                                              "   "         "          "   Me   Me     CH                                2.470                                                                              "   COCH.sub. 2 CH.sub.3                                                                     "          "   OMe  OMe    CH                                2.471                                                                              Et  CHO       "          "   "    "      CH                                2.472                                                                              Pr  "         "          "   "    "      CH                                2.473                                                                              Et  COCH.sub.3                                                                               "          "   "    "      CH                                2.474                                                                              Pr  "         "          "   "    "      CH                                2.475                                                                              Et  COCH.sub.2 CH.sub.3                                                                      "          "   "    "      CH                                2.476                                                                              Me                                                                                  ##STR26##                                                                               "          "   "    "      CH                                2.477                                                                              Me  CO.sub.2 Me                                                                              "          "   "    "      CH                                2.478                                                                              Et  "         "          "   "    "      CH                                2.479                                                                              Pr  "         "          "   "    "      CH                                2.480                                                                              Me  CONHEt    "          "   "    "      CH                                2.481                                                                              Et  "         "          "   "    "      CH                                2.482                                                                              Pr  "         "          "   "    "      CH                                2.483                                                                              Me  CHO       CO.sub.2 CH.sub.2 CH.sub.2 Cl                                                             H   OMe  OMe    CH                                2.484                                                                              "   "         "          "   OMe  Me     N                                 2.485                                                                              "   "         "          "   Me   Me     CH                                2.486                                                                              "   COCH.sub.3                                                                               "          "   OMe  OMe    CH                                2.487                                                                              "   "         "          "   OMe  Me     N                                 2.488                                                                              "   "         "          "   Me   Me     CH                                2.489                                                                              "   COCH.sub.2 CH.sub.3                                                                      "          "   OMe  OMe    CH                                2.490                                                                              Et  CHO       "          "   "    "      "                                 2.491                                                                              Pr  "         "          "   "    "      "                                 2.492                                                                              Et  COCH.sub.3                                                                               "          "   "    "      "                                 2.493                                                                              Pr  "         "          "   "    "      "                                 2.494                                                                              Et  COCH.sub.2 CH.sub.3                                                                      "          "   "    "      "                                 2.495                                                                              Me                                                                                  ##STR27##                                                                               "          "   "    "      "                                 2.496                                                                              Me  CO.sub.2 Me                                                                              "          "   "    "      "                                 2.497                                                                              Et  "         "          "   "    "      "                                 2.498                                                                              Pr  "         "          "   "    "      "                                 2.499                                                                              Me  CONHEt    "          "   "    "      "                                 2.500                                                                              Et  "         "          "   "    "      "                                 2.501                                                                              Pr  "         "          "   "    "      "                                 2.502                                                                              Me  CHO       CO.sub.2 (CH.sub.2).sub.2 OMe                                                             H   OMe  OMe    CH                                2.503                                                                              "   "         "          H   OMe  Me     N                                 2.504                                                                              "   "         "          "   Me   Me     CH                                2.505                                                                              "   COCH.sub.3                                                                               "          "   OMe  OMe    CH                                2.506                                                                              "   "         "          "   OMe  Me     N                                 2.507                                                                              "   "         "          "   Me   Me     CH                                2.508                                                                              "   COCH.sub.2 CH.sub.3                                                                      "          "   OMe  OMe    CH                                2.509                                                                              Et  CHO       "          "   "    "      "                                 2.510                                                                              Pr  "         "          "   "    "      "                                 2.511                                                                              Et  COCH.sub.3                                                                               "          "   "    "      "                                 2.512                                                                              Pr  "         "          "   "    "      "                                 2.513                                                                              Et  COCH.sub.2 CH.sub.3                                                                      "          "   "    "      "                                 2.514                                                                              Me                                                                                  ##STR28##                                                                               "          "   "    "      "                                 2.515                                                                              Me  CO.sub.2 Me                                                                              "          "   "    "      "                                 2.516                                                                              Et  "         "          "   "    "      "                                 2.517                                                                              Pr  "         "          "   "    "      "                                 2.518                                                                              Me  CONHEt    "          "   "    "      "                                 2.519                                                                              Et  "         "          "   "    "      "                                 2.520                                                                              Pr  "         "          "   "    "      "                                 2.521                                                                              Me  CHO       CO.sub.2 CH.sub.2 CCl.sub.3                                                               H   OMe  OMe    CH                                2.522                                                                              "   "         "          H   OMe  Me     N                                 2.523                                                                              "   "         "          "   Me   Me     CH                                2.524                                                                              "   COCH.sub.3                                                                               "          "   OMe  OMe    CH                                2.525                                                                              "   "         "          "   OMe  Me     N                                 2.526                                                                              "   "         "          "   Me   Me     CH                                2.527                                                                              "   COCH.sub.2 CH.sub.3                                                                      "          "   OMe  OMe    CH                                2.528                                                                              Et  CHO       "          "   "    "      "                                 2.529                                                                              Pr  "         "          "   "    "      "                                 2.530                                                                              Et  COCH.sub.3                                                                               "          "   "    "      "                                 2.531                                                                              Pr  "         "          "   "    "      "                                 2.532                                                                              Et  COCH.sub.2 CH.sub.3                                                                      "          "   "    "      "                                 2.533                                                                              Me                                                                                  ##STR29##                                                                               "          "   "    "      "                                 2.534                                                                              Me  CO.sub.2 Me                                                                              "          "   "    "      "                                 2.535                                                                              Et  "         "          "   "    "      "                                 2.536                                                                              Pr  "         "          "   "    "      "                                 2.537                                                                              Me  CONHEt    "          "   "    "      "                                 2.538                                                                              Et  "         "          "   "    "      "                                 2.539                                                                              Pr  "         "          "   "    "      "                                 __________________________________________________________________________

    __________________________________________________________________________     No. R.sup.1                                                                            R.sup.2   R.sup.3    R.sup.4                                                                            X    Y      Z   m.p.                          __________________________________________________________________________     2.540                                                                              Me  CHO       CO.sub.2 CH.sub.2 CCH                                                                     H   OMe  OMe    CH                                2.541                                                                              "   "         "          H   OMe  Me     N                                 2.542                                                                              "   "         "          "   Me   Me     CH                                2.543                                                                              "   COCH.sub.3                                                                               "          "   OMe  OMe    CH                                2.544                                                                              "   "         "          "   OMe  Me     N                                 2.545                                                                              "   "         "          "   Me   Me     CH                                2.546                                                                              "   COCH.sub.2 CH.sub.3                                                                      "          "   OMe  OMe    CH                                2.547                                                                              Et  CHO       "          "   "    "      "                                 2.548                                                                              Pr  "         "          "   "    "      "                                 2.549                                                                              Et  COCH.sub.3                                                                               "          "   "    "      "                                 2.550                                                                              Pr  "         "          "   "    "      "                                 2.551                                                                              Et  COCH.sub.2 CH.sub.3                                                                      "          "   "    "      "                                 2.552                                                                              Me                                                                                  ##STR30##                                                                               "          "   "    "      "                                 2.553                                                                              Me  CO.sub.2 Me                                                                              "          "   "    "      "                                 2.554                                                                              Et  "         "          "   "    "      "                                 2.555                                                                              Pr  "         "          "   "    "      "                                 2.556                                                                              Me  CONHEt    "          "   "    "      "                                 2.557                                                                              Et  "         "          "   "    "      "                                 2.558                                                                              Pr  "         "          "   "    "      "                                 2.559                                                                              Me  SO.sub.2 Et                                                                              CO.sub.2 Me                                                                               H   OMe  OMe    CH                                2.560                                                                              "   "         "          "   "    OMe    N                                 2.561                                                                              "   "         "          "   "    Me     N                                 2.562                                                                              "   "         "          "   "    "      CH                                2.563                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.                                                                     N                                 2.564                                                                              "   "         "          "   Me   Me     CH                                2.565                                                                              "   "         "          "   "    "      N                                 2.566                                                                              "   "         "          "   Cl   OMe    CH                                2.567                                                                              "   "         "          Me  OMe  OMe    CH                                2.568                                                                              "   "         "          "   "    Me     N                                 2.569                                                                              "   "         CO.sub.2 Et                                                                               H   OMe  OMe    CH                                2.570                                                                              "   "         "          "   "    Cl     CH                                2.571                                                                              "   "         "          "   Me   Me     CH                                2.572                                                                              "   "         "          "   OMe  Me     N                                 2.573                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 2.574                                                                              "   "         "          Me  OMe  OMe    CH                                2.575                                                                              "   "         "          "   OMe  Me     N                                 2.576                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                2.577                                                                              "   "         "          "   "    "      N                                 2.578                                                                              "   "         "          "   OMe  Me     N                                 2.579                                                                              "   "         "          "   Me   Me     CH                                2.580                                                                              "   "         "          "   OMe  Cl     CH                                2.581                                                                              "   "         "          Me  Me   OMe    N                                 2.582                                                                              "   "         "          "   OMe  OMe    CH                                2.583                                                                              Me  SO.sub.2 Et                                                                              CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                2.584                                                                              "   "         "          "   "    "      N                                 2.585                                                                              "   "         "          "   OMe  Me     N                                 2.586                                                                              "   "         "          "   OMe  Cl     CH                                2.587                                                                              "   "         "          "   Me   Me     CH                                2.588                                                                              "   "         "          "   SMe  NEt.sub.2                                                                             N                                 2.589                                                                              "   "         CO.sub.2 -i-Pr                                                                            Me  OMe  Me     N                                 2.590                                                                              "   "         "          "   OMe  OMe    CH                                2.591                                                                              Me  "         CO.sub.2 -allyl                                                                           H   OMe  OMe    CH                                2.592                                                                              Et  "         CO.sub.2 Me                                                                               H   OMe  OMe    CH                                2.593                                                                              "   "         "          H   OMe  Me     N                                 2.594                                                                              "   "         "          "   Me   Me     CH                                2.595                                                                              "   "         "          "   Cl   OMe    CH                                2.596                                                                              "   "         "          Me  OMe  OMe    CH                                2.597                                                                              "   "         "          "   OMe  Me     N                                 2.598                                                                              "   "         CO.sub.2 Et                                                                               H   OMe  OMe    CH                                2.599                                                                              "   "         "          "   OMe  Me     CH                                2.600                                                                              "   "         "          "   Cl   OMe    CH                                2.601                                                                              "   "         "          "   OMe  Me     N                                 2.602                                                                              "   "         "          Me  OMe  OMe    CH                                2.603                                                                              "   "         "          "   "    Me     N                                 2.604                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                2.605                                                                              "   "         "          "   OMe  Me     N                                 2.606                                                                              "   "         "          "   OMe  Cl     CH                                2.607                                                                              "   "         "          "   Me   Me     CH                                2.608                                                                              "   "         "          Me  OMe  OMe    CH                                2.609                                                                              "   "         "          "   OMe  Me     N                                 2.610                                                                              "   "         CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                2.611                                                                              "   "         "          "   OMe  Me     N                                 2.612                                                                              "   "         "          "   Me   Me     CH                                2.613                                                                              "   "         "          Me  OMe  Me     N                                 2.614                                                                              n-Pr                                                                               SO.sub.2 Et                                                                              CO.sub.2 Me                                                                               H   OMe  OMe    CH                                2.615                                                                              "   "         "          "   "    Cl     CH                                2.616                                                                              "   "         "          "   Me   Me     CH                                2.617                                                                              "   "         "          "   OMe  Me     N                                 2.618                                                                              "   "         "          Me  OMe  OMe    CH                                2.619                                                                              "   "         "          "   OMe  Me     N                                 2.620                                                                              n-Pr                                                                               "         CO.sub.2 Et                                                                               H   "    "      N                                 2.621                                                                              "   "         "          "   "    OMe    CH                                2.622                                                                              "   "         "          "   Me   Me     CH                                2.623                                                                              "   "         CO.sub.2 -n-Pr                                                                            "   OMe  OMe    CH                                2.624                                                                              i-Pr                                                                               "         CO.sub.2 Me                                                                               H   "    "      CH                                2.625                                                                              "   "         "          "   "    Me     N                                 2.626                                                                              "   "         "          "   Me   Me     CH                                2.627                                                                              "   "         "          "   Cl   OMe    N                                 2.628                                                                              "   "         "          Me  OMe  Me     N                                 2.629                                                                              "   "         "          "   "    OMe    CH                                2.630                                                                              Allyl                                                                              "         CO.sub.2 Me                                                                               H   OMe  OMe    CH                                2.631                                                                              "   "         "          "   "    Cl     CH                                2.632                                                                              "   "         "          "   Me   Me     CH                                2.633                                                                              "   "         "          "   OMe  Me     N                                 2.634                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                2.635                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                2.636                                                                              "   "         CO.sub.2 -i-Pr                                                                            "   "    "      CH                                2.637                                                                              Me  SO.sub.2 CH.sub.2 Cl                                                                     CO.sub.2Me H   OMe  OMe    CH                                2.638                                                                              "   "         "          "   "    OMe    N                                 2.639                                                                              "   "         "          "   "    Me     N                                 2.640                                                                              "   "         "          "   "    "      CH                                2.641                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 2.642                                                                              "   "         "          "   Me   Me     CH                                2.643                                                                              "   "         "          "   "    "      N                                 2.644                                                                              "   "         "          "   Cl   OMe    CH                                2.645                                                                              "   "         "          Me  OMe  OMe    CH                                2.646                                                                              "   "         "          "   "    Me     N                                 2.647                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                2.648                                                                              "   "         "          "   "    Cl     CH                                2.649                                                                              "   "         "          "   Me   Me     CH                                2.650                                                                              "   "         "          "   OMe  Me     N                                 2.651                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 2.652                                                                              "   "         "          Me  OMe  OMe    CH                                2.653                                                                              "   "         "          "   OMe  Me     N                                 2.654                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                2.655                                                                              "   "         "          "   "    "      N                                 2.656                                                                              "   "         "          "   OMe  Me     N                                 2.657                                                                              "   "         "          "   Me   Me     CH                                2.658                                                                              "   "         "          "   OMe  Cl     CH                                2.659                                                                              "   "         "          Me  Me   OMe    N                                 2.660                                                                              "   "         "          "   OMe  OMe    CH                                2.661                                                                              Me  SO.sub.2 CH.sub.2 Cl                                                                     CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                2.662                                                                              "   "         "          "   "    "      N                                 2.663                                                                              "   "         "          "   OMe  Me     N                                 2.664                                                                              "   "         "          "   OMe  Cl     CH                                2.665                                                                              "   "         "          "   Me   Me     CH                                2.666                                                                              "   "         "          "   SMe  NEt.sub.2                                                                             N                                 2.667                                                                              "   "         CO.sub.2 -i-Pr                                                                            Me  OMe  Me     N                                 2.668                                                                              "   "         "          "   OMe  OMe    CH                                2.669                                                                              Me  "         CO.sub.2 -Allyl                                                                           H   OMe  OMe    CH                                2.670                                                                              Et  "         CO.sub.2Me H   OMe  OMe    CH                                2.671                                                                              "   "         "          H   OMe  Me     N                                 2.672                                                                              "   "         "          "   Me   Me     CH                                2.673                                                                              "   "         "          "   Cl   OMe    CH                                2.674                                                                              "   "         "          Me  OMe  OMe    CH                                2.675                                                                              "   "         "          "   OMe  Me     N                                 2.676                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                2.677                                                                              "   "         "          "   OMe  Me     CH                                2.678                                                                              "   "         "          "   Cl   OMe    CH                                2.679                                                                              "   "         "          "   OMe  Me     N                                 2.680                                                                              "   "         "          Me  OMe  OMe    CH                                2.681                                                                              "   "         "          "   "    Me     N                                 2.682                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                2.683                                                                              "   "         "          "   OMe  Me     N                                 2.684                                                                              "   "         "          "   OMe  Cl     CH                                2.685                                                                              "   "         "          "   Me   Me     CH                                2.686                                                                              "   "         "          Me  OMe  OMe    CH                                2.687                                                                              "   "         "          "   "    Me     N                                 2.688                                                                              "   "         CO.sub.2 i-Pr                                                                             H   OMe  OMe    CH                                2.689                                                                              "   "         "          "   OMe  Me     N                                 2.690                                                                              "   "         "          "   Me   Me     CH                                2.691                                                                              "   "         "          Me  OMe  Me     N                                 2.692                                                                              n-Pr                                                                               SO.sub.2 CH.sub.2 Cl                                                                     CO.sub.2Me H   OMe  OMe    CH                                2.693                                                                              "   "         "          "   "    Cl     CH                                2.694                                                                              "   "         "          "   Me   Me     CH                                2.695                                                                              "   "         "          "   OMe  Me     N                                 2.696                                                                              "   "         "          Me  OMe  OMe    CH                                2.697                                                                              "   "         "          "   "    Me     N                                 2.698                                                                              n-Pr                                                                               "         CO.sub.2Et H   "    "      N                                 2.699                                                                              "   "         "          "   "    OMe    CH                                2.700                                                                              "   "         "          "   Me   Me     CH                                2.701                                                                              "   "         CO.sub.2 -n-Pr                                                                            "   OMe  OMe    CH                                2.702                                                                              i-Pr                                                                               "         CO.sub.2Me H   OMe  OMe    CH                                2.703                                                                              "   "         "          "   OMe  Me     N                                 2.704                                                                              "   "         "          "   Me   Me     CH                                2.705                                                                              "   "         "          "   Cl   OMe    N                                 2.706                                                                              "   "         "          Me  OMe  Me     N                                 2.707                                                                              "   "         "          "   "    OMe    CH                                2.708                                                                              Allyl                                                                              "         CO.sub.2Me H   OMe  OMe    CH                                2.709                                                                              "   "         "          "   "    Cl     CH                                2.710                                                                              "   "         "          "   Me   Me     CH                                2.711                                                                              "   "         "          "   OMe  Me     N                                 2.712                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                2.713                                                                              "   "         CO.sub.2 -n-Pr                                                                            "   "    "      CH                                2.714                                                                              "   "         CO.sub.2 -i-Pr                                                                            "   "    "      CH                                2.715                                                                              Me  SO.sub.2 CH.sub.3                                                                        CO.sub.2Me H   OMe  OMe    CH  119° C.                2.716                                                                              "   "         "          "   "    OMe    N                                 2.717                                                                              "   "         "          "   "    Me     N                                 2.718                                                                              "   "         "          "   "    "      CH                                2.719                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 2.720                                                                              "   "         "          "   Me   Me     CH                                2.721                                                                              "   "         "          "   "    "      N                                 2.722                                                                              "   "         "          "   Cl   OMe    CH                                2.723                                                                              "   "         "          Me  OMe  OMe    CH                                2.724                                                                              "   "         "          "   "    Me     N                                 2.725                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                2.726                                                                              "   "         "          "   "    Cl     CH                                2.727                                                                              "   "         "          "   Me   Me     CH                                2.728                                                                              "   "         "          "   OMe  Me     N                                 2.729                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 2.730                                                                              "   "         "          Me  OMe  OMe    CH                                2.731                                                                              "   "         "          "   OMe  Me     N                                 2.732                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                2.733                                                                              "   "         "          "   "    "      N                                 2.734                                                                              "   "         "          "   OMe  Me     N                                 2.735                                                                              "   "         "          "   Me   Me     CH                                2.736                                                                              "   "         "          "   OMe  Cl     CH                                2.737                                                                              "   "         "          Me  Me   OMe    N                                 2.738                                                                              "   "         "          "   OMe  OMe    CH                                2.739                                                                              Me  SO.sub.2 Me                                                                              CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                2.740                                                                              "   "         "          "   "    "      N                                 2.741                                                                              "   "         "          "   OMe  Me     N                                 2.742                                                                              "   "         "          "   OMe  Cl     CH                                2.743                                                                              "   "         "          "   Me   Me     CH                                2.744                                                                              "   "         "          "   SMe  NEt.sub.2                                                                             N                                 2.745                                                                              "   "         CO.sub.2 -i-Pr                                                                            Me  OMe  Me     N                                 2.746                                                                              "   "         "          "   OMe  OMe    CH                                2.747                                                                              Me  "         CO.sub.2 -Allyl                                                                           H   OMe  OMe    CH                                2.748                                                                              Et  "         CO.sub.2Me H   OMe  OMe    CH                                2.749                                                                              "   "         "          H   OMe  Me     N                                 2.750                                                                              "   "         "          "   Me   Me     CH                                2.751                                                                              "   "         "          "   Cl   OMe    CH                                2.752                                                                              "   "         "          Me  OMe  OMe    CH                                2.753                                                                              "   "         "          "   OMe  Me     N                                 2.754                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                2.755                                                                              "   "         "          "   OMe  Me     CH                                2.756                                                                              "   "         "          "   Cl   OMe    CH                                2.757                                                                              "   "         "          "   OMe  Me     N                                 2.758                                                                              "   "         "          Me  OMe  OMe    CH                                2.759                                                                              "   "         "          "   "    Me     N                                 2.760                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                2.761                                                                              "   "         "          "   OMe  Me     N                                 2.762                                                                              "   "         "          "   OMe  Cl     CH                                2.763                                                                              "   "         "          "   Me   Me     CH                                2.764                                                                              "   "         "          Me  OMe  OMe    CH                                2.765                                                                              "   "         "          "   OMe  Me     N                                 2.766                                                                              "   "         CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                2.767                                                                              "   "         "          "   OMe  Me     N                                 2.768                                                                              "   "         "          "   Me   Me     CH                                2.769                                                                              "   "         "          Me  OMe  Me     N                                 2.770                                                                              n-Pr                                                                               SO.sub.2 Me                                                                              CO.sub.2Me H   OMe  OMe    CH                                2.771                                                                              "   "         "          "   "    Cl     CH                                2.772                                                                              "   "         "          "   Me   Me     CH                                2.773                                                                              "   "         "          "   OMe  Me     N                                 2.774                                                                              "   "         "          Me  OMe  OMe    CH                                2.775                                                                              "   "         "          "   OMe  Me     N                                 2.776                                                                              n-Pr                                                                               "         CO.sub.2Et H   "    "      N                                 2.777                                                                              "   "         "          "   "    OMe    CH                                2.778                                                                              "   "         "          "   Me   Me     CH                                2.779                                                                              "   "         CO.sub.2 -n-Pr                                                                            "   OMe  OMe    CH                                2.780                                                                              i-Pr                                                                               "         CO.sub.2Me H   OMe  OMe    CH                                2.781                                                                              "   "         "          "   OMe  Me     N                                 2.782                                                                              "   "         "          "   Me   Me     CH                                2.783                                                                              "   "         "          "   Cl   OMe    N                                 2.784                                                                              "   "         "          Me  OMe  Me     N                                 2.785                                                                              "   "         "          "   "    OMe    CH                                2.786                                                                              Allyl                                                                              "         CO.sub.2Me H   OMe  OMe    CH                                2.787                                                                              "   "         "          "   "    Cl     CH                                2.788                                                                              Allyl                                                                              "         CO.sub.2Me H   OMe  OMe    CH                                2.789                                                                              "   "         "          "   "    Cl     CH                                2.790                                                                              "   "         "          "   Me   Me     CH                                2.791                                                                              "   "         "          "   OMe  Me     N                                 2.792                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                2.793                                                                              "   "         CO.sub.2 -n-Pr                                                                            "   "    "      CH                                2.794                                                                              "   "         CO.sub.2 -i-Pr                                                                            "   "    "      CH                                2.795                                                                              Me  CONH      CO.sub.2Me H   OMe  OMe    CH                                        CH.sub.2 CH.sub.2 Cl                                                   2.796                                                                              "   CONH      "          "   "    OMe    N                                         CH.sub.2 CH.sub.2 Cl                                                   2.797                                                                              "   CONH      "          "   "    Me     N                                         CH.sub.2 CH.sub.2 Cl                                                   2.798                                                                              "   CONH      "          "   "    "      CH                                        CH.sub.2 CH.sub.2 Cl                                                   2.799                                                                              "   CONH      "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                         CH.sub.2 CH.sub.2 Cl                                                   2.800                                                                              "   CONH      "          "   Me   Me     CH                                        CH.sub.2 CH.sub. 2 Cl                                                  2.801                                                                              "   CONH      "          "   "    "      N                                         CH.sub.2 CH.sub.2 Cl                                                   2.802                                                                              "   CONH      "          "   Cl   OMe    CH                                        CH.sub.2 CH.sub.2 Cl                                                   2.803                                                                              "   CONH      "          Me  OMe  OMe    CH                                        CH.sub.2 CH.sub.2 Cl                                                   2.804                                                                              "   CONH      "          "   "    Me     N                                         CH.sub.2 CH.sub.2 Cl                                                   2.805                                                                              "   CONH      CO.sub.2Et H   OMe  OMe    CH                                        CH.sub.2 CH.sub.2 Cl                                                   2.806                                                                              "   CONH      "          "   "    Cl     CH                                        CH.sub.2 CH.sub.2 Cl                                                   2.807                                                                              "   CONH      "          "   Me   Me     CH                                        CH.sub.2 CH.sub.2 Cl                                                   2.808                                                                              "   CONH      "          "   OMe  Me     N                                         CH.sub.2 CH.sub.2 Cl                                                   2.809                                                                              "   CONH      "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                         CH.sub.2 CH.sub.2 Cl                                                   2.810                                                                              "   CONH      "          Me  OMe  OMe    CH                                        CH.sub.2 CH.sub.2 Cl                                                   2.811                                                                              "   CONH      "          "   OMe  Me     N                                         CH.sub.2 CH.sub.2 Cl                                                   2.812                                                                              "   CONH      CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                        CH.sub.2 CH.sub.2 Cl                                                   2.813                                                                              "   CONH      "          "   "    "      N                                         CH.sub.2 CH.sub.2 Cl                                                   2.814                                                                              "   CONH      "          "   OMe  Me     N                                         CH.sub.2 CH.sub.2 Cl                                                   2.815                                                                              "   CONH      "          "   Me   Me     CH                                        CH.sub.2 CH.sub.2 Cl                                                   2.816                                                                              "   CONH      "          "   OMe  Cl     CH                                        CH.sub.2 CH.sub.2 Cl                                                   2.817                                                                              "   CONH      "          Me  Me   OMe    N                                         CH.sub.2 CH.sub.2 Cl                                                   2.818                                                                              "   CONH      "          "   OMe  OMe    CH                                        CH.sub.2 CH.sub.2 Cl                                                   2.819                                                                              Me  CO        CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                        NHCH.sub.2 CH.sub.2 Cl                                                 2.820                                                                              "   CO        "          "   "    "      N                                         NHCH.sub.2 CH.sub.2 Cl                                                 2.821                                                                              "   CO        "          "   OMe  Me     N                                         NHCH.sub.2 CH.sub.2 Cl                                                 2.822                                                                              "   CO        "          "   OMe  Cl     CH                                        NHCH.sub.2 CH.sub.2 Cl                                                 2.823                                                                              "   CO        "          "   Me   Me     CH                                        NHCH.sub.2 CH.sub.2 Cl                                                 2.824                                                                              "   CO        "          "   SMe  NEt.sub.2                                                                             N                                         NHCH.sub.2 CH.sub.2 Cl                                                 2.825                                                                              "   CO        CO.sub.2 -i-Pr                                                                            Me  OMe  Me     N                                         NHCH.sub.2 CH.sub.2 Cl                                                 2.826                                                                              "   CO        "          "   OMe  OMe    CH                                        NHCH.sub.2 CH.sub.2 Cl                                                 2.827                                                                              Me  CO        CO.sub.2 -Allyl                                                                           H   OMe  OMe    CH                                        NHCH.sub.2 CH.sub.2 Cl                                                 2.828                                                                              Et  CO        CO.sub.2Me H   OMe  OMe    CH                                        NHCH.sub.2 CH.sub.2 Cl                                                 2.829                                                                              "   CO        "          H   OMe  Me     N                                         NHCH.sub.2 CH.sub.2 Cl                                                 2.830                                                                              "   CO        "          "   Me   Me     CH                                        NHCH.sub.2 CH.sub.2 Cl                                                 2.831                                                                              "   CO        "          "   Cl   OMe    CH                                        NHCH.sub.2 CH.sub.2 Cl                                                 2.832                                                                              "   CO        "          Me  OMe  OMe    CH                                        NHCH.sub.2 CH.sub.2 Cl                                                 2.833                                                                              "   CO        "          "   OMe  Me     N                                         NHCH.sub.2 CH.sub.2 Cl                                                 2.834                                                                              "   CO        CO.sub.2Et H   OMe  OMe    CH                                        NHCH.sub.2 CH.sub.2 Cl                                                 2.835                                                                              "   CO        "          "   OMe  Me     CH                                        NHCH.sub.2 CH.sub.2 Cl                                                 2.836                                                                              "   CO        "          "   Cl   OMe    CH                                        NHCH.sub.2 CH.sub.2 Cl                                                 2.837                                                                              "   CO        "          "   OMe  Me     N                                         NHCH.sub.2 CH.sub.2 Cl                                                 2.838                                                                              "   CO        "          Me  OMe  OMe    CH                                        NHCH.sub. 2 CH.sub.2 Cl                                                2.839                                                                              "   CO        "          "   "    Me     N                                         NHCH.sub.2 CH.sub.2 Cl                                                 2.840                                                                              "   CO        CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                        NHCH.sub.2 CH.sub.2 Cl                                                 2.841                                                                              "   CO        "          H   OMe  Me     N                                         NHCH.sub.2 CH.sub.2 Cl                                                 2.842                                                                              "   CO        "          "   OMe  Cl     CH                                        NHCH.sub.2 CH.sub.2 Cl                                                 2.843                                                                              "   CO        "          "   Me   Me     CH                                        NHCH.sub.2 CH.sub.2 Cl                                                 2.844                                                                              "   CO        "          Me  OMe  OMe    CH                                        NHCH.sub.2 CH.sub.2 Cl                                                 2.845                                                                              "   CO        "          "   OMe  Me     N                                         NHCH.sub.2 CH.sub.2 Cl                                                 2.846                                                                              "   CO        CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                        NHCH.sub.2 CH.sub.2 Cl                                                 2.847                                                                              "   CO        "          H   OMe  Me     N                                         NHCH.sub.2 CH.sub.2 Cl                                                 2.848                                                                              "   CO        "          "   Me   Me     CH                                        NHCH.sub.2 CH.sub.2 Cl                                                 2.849                                                                              "   CO        "          Me  OMe  Me     N                                         NHCH.sub.2 CH.sub.2 Cl                                                 2.850                                                                              n-Pr                                                                               CONH      CO.sub.2Me H   OMe  OMe    CH                                        CH.sub.2 CH.sub.2 Cl                                                   2.851                                                                              "   CONH      "          "   "    Cl     CH                                        CH.sub.2 CH.sub.2 Cl                                                   2.852                                                                              "   CONH      "          "   Me   Me     CH                                        CH.sub.2 CH.sub.2 Cl                                                   2.853                                                                              "   CONH      "          "   OMe  Me     N                                         CH.sub.2 CH.sub.2 Cl                                                   2.854                                                                              "   CONH      "          Me  OMe  OMe    CH                                        CH.sub.2 CH.sub.2 Cl                                                   2.855                                                                              "   CONH      "          "   OMe  Me     N                                         CH.sub.2 CH.sub.2 Cl                                                   2.856                                                                              n-Pr                                                                               CONH      CO.sub.2Et H   "    "      N                                         CH.sub.2 CH.sub.2 Cl                                                   2.857                                                                              "   CONH      "          "   "    OMe    CH                                        CH.sub.2 CH.sub.2 Cl                                                   2.858                                                                              "   CONH      "          "   Me   Me     CH                                        CH.sub.2 CH.sub.2 Cl                                                   2.859                                                                              "   CONH      CO.sub.2 -n-Pr                                                                            "   OMe  OMe    CH                                        CH.sub.2 CH.sub.2 Cl                                                   2.860                                                                              i-Pr                                                                               CONH      CO.sub.2Me H   OMe  OMe    CH                                        CH.sub.2 CH.sub.2 Cl                                                   2.861                                                                              "   CONH      "          "   OMe  Me     N                                         CH.sub.2 CH.sub.2 Cl                                                   2.862                                                                              "   CONH      "          "   Me   Me     CH                                        CH.sub.2 CH.sub.2 Cl                                                   2.863                                                                              "   CONH      "          "   Cl   OMe    N                                         CH.sub.2 CH.sub.2 Cl                                                   2.864                                                                              "   CONH      "          Me  OMe  Me     N                                         CH.sub.2 CH.sub.2 Cl                                                   2.865                                                                              "   CONH      "          "   "    OMe    CH                                        CH.sub.2 CH.sub.2 Cl                                                   2.866                                                                              Allyl                                                                              CONH      CO.sub.2Me H   OMe  OMe    CH                                        CH.sub.2 CH.sub.2 Cl                                                   2.867                                                                              "   CONH      "          "   "    Cl     CH                                        CH.sub.2 CH.sub.2 Cl                                                   2.868                                                                              "   CONH      "          "   Me   Me     CH                                        CH.sub.2 CH.sub.2 Cl                                                   2.869                                                                              "   CONH      "          "   OMe  Me     N                                         CH.sub.2 CH.sub.2 Cl                                                   2.870                                                                              "   CONH      CO.sub.2Et H   OMe  OMe    CH                                        CH.sub.2 CH.sub.2 Cl                                                   2.871                                                                              "   CONH      CO.sub.2 -n-Pr                                                                            "   "    "      CH                                        CH.sub.2 CH.sub.2 Cl                                                   2.872                                                                              "   CONH      CO.sub.2 -i-Pr                                                                            "   "    "      CH                                        CH.sub.2 CH.sub.2 Cl                                                   2.873                                                                              Me  COOCH.sub.2 CCl.sub.3                                                                    CO.sub.2Me H   OMe  OMe    CH                                2.874                                                                              "   "         "          "   "    OMe    N                                 2.875                                                                              "   "         "          "   "    Me     N                                 2.876                                                                              "   "         "          "   "    "      CH                                2.877                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 2.878                                                                              "   "         "          "   Me   Me     CH                                2.879                                                                              "   "         "          "   "    "      N                                 2.880                                                                              "   "         "          "   Cl   OMe    CH                                2.881                                                                              "   "         "          Me  OMe  OMe    CH                                2.882                                                                              "   "         "          "   "    Me     N                                 2.883                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                2.884                                                                              "   "         "          "   "    Cl     CH                                2.885                                                                              "   "         "          "   Me   Me     CH                                2.886                                                                              "   "         "          "   OMe  Me     N                                 2.887                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 2.888                                                                              "   "         "          Me  OMe  OMe    CH                                2.889                                                                              "   "         "          "   OMe  Me     N                                 2.890                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                2.891                                                                              "   "         "          "   "    "      N                                 2.892                                                                              "   "         "          "   OMe  Me     N                                 2.893                                                                              "   "         "          "   Me   Me     CH                                2.894                                                                              "   "         "          "   OMe  Cl     CH                                2.895                                                                              "   "         "          Me  Me   OMe    N                                 2.896                                                                              "   "         "          "   OMe  OMe    CH                                2.897                                                                              Me  COOCH.sub.2 CCl.sub.3                                                                    CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                2.898                                                                              "   "         "          "   "    "      N                                 2.899                                                                              "   "         "          "   OMe  Me     N                                 2.900                                                                              "   "         "          "   OMe  Cl     CH                                2.901                                                                              "   "         "          "   Me   Me     CH                                2.902                                                                              "   "         "          "   SMe  NEt.sub.2                                                                             N                                 2.903                                                                              "   "         CO.sub.2 -i-Pr                                                                            Me  OMe  Me     N                                 2.904                                                                              "   "         "          "   OMe  OMe    CH                                2.905                                                                              Me  "         CO.sub.2 -Allyl                                                                           H   OMe  OMe    CH                                2.906                                                                              Et  "         CO.sub.2Me H   OMe  OMe    CH                                2.907                                                                              "   "         "          H   OMe  Me     N                                 2.908                                                                              "   "         "          "   Me   Me     CH                                2.909                                                                              "   "         "          "   Cl   OMe    CH                                2.910                                                                              "   "         "          Me  OMe  OMe    CH                                2.911                                                                              "   "         "          "   OMe  Me     N                                 2.912                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                2.913                                                                              "   "         "          "   OMe  Me     CH                                2.914                                                                              "   "         "          "   Cl   OMe    CH                                2.915                                                                              "   "         "          "   OMe  Me     N                                 2.916                                                                              "   "         "          Me  OMe  OMe    CH                                2.917                                                                              "   "         "          "   "    Me     N                                 2.918                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                2.919                                                                              "   "         "          "   OMe  Me     N                                 2.920                                                                              "   "         "          "   OMe  Cl     CH                                2.921                                                                              "   "         "          "   Me   Me     CH                                2.922                                                                              "   "         "          Me  OMe  OMe    CH                                2.923                                                                              "   "         "          "   OMe  Me     N                                 2.924                                                                              "   "         CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                2.925                                                                              "   "         "          "   OMe  Me     N                                 2.926                                                                              "   "         "          "   Me   Me     CH                                2.927                                                                              "   "         "          Me  OMe  Me     N                                 2.928                                                                              n-Pr                                                                               COOCH.sub.2 CCl.sub.3                                                                    CO.sub.2Me H   OMe  OMe    CH                                2.929                                                                              "   "         "          "   "    Cl     CH                                2.930                                                                              "   "         "          "   Me   Me     CH                                2.931                                                                              "   "         "          "   OMe  Me     N                                 2.932                                                                              "   "         "          Me  OMe  OMe    CH                                2.933                                                                              "   "         "          "   OMe  Me     N                                 2.934                                                                              n-Pr                                                                               "         CO.sub.2Et H   OMe  Me     N                                 2.935                                                                              "   "         "          "   "    OMe    CH                                2.936                                                                              "   "         "          "   Me   Me     CH                                2.937                                                                              "   "         CO.sub.2 -n-Pr                                                                            "   OMe  OMe    CH                                2.938                                                                              i-Pr                                                                               "         CO.sub.2Me H   OMe  OMe    CH                                2.939                                                                              "   "         "          "   OMe  Me     N                                 2.940                                                                              "   "         "          "   Me   Me     CH                                2.941                                                                              "   "         "          "   Cl   OMe    N                                 2.942                                                                              "   "         "          Me  OMe  Me     N                                 2.943                                                                              "   "         "          "   "    OMe    CH                                2.944                                                                              Allyl                                                                              "         CO.sub.2Me H   OMe  OMe    CH                                2.945                                                                              "   "         "          "   "    Cl     CH                                2.946                                                                              "   "         "          "   Me   Me     CH                                2.947                                                                              "   "         "          "   OMe  Me     N                                 2.948                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                2.949                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                2.950                                                                              "   "         CO.sub.2 -i-Pr                                                                            "   "    "      CH                                2.951                                                                              Me  COCH.sub.2 Br                                                                            CO.sub.2Me H   OMe  OMe    CH                                2.952                                                                              "   "         "          "   "    OMe    N                                 2.953                                                                              "   "         "          "   "    Me     N                                 2.954                                                                              "   "         "          "   "    "      CH                                2.955                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 2.956                                                                              "   "         "          "   Me   Me     CH                                2.957                                                                              "   "         "          "   "    "      N                                 2.958                                                                              "   "         "          "   Cl   OMe    CH                                2.959                                                                              "   "         "          Me  OMe  OMe    CH                                2.960                                                                              "   "         "          "   "    Me     N                                 2.961                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                2.962                                                                              "   "         "          "   "    Cl     CH                                2.963                                                                              "   "         "          "   Me   Me     CH                                2.964                                                                              "   "         "          "   OMe  Me     N                                 2.965                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 2.966                                                                              "   "         "          Me  OMe  OMe    CH                                2.967                                                                              "   "         "          "   OMe  Me     N                                 2.968                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                2.969                                                                              "   "         "          "   "    "      N                                 2.970                                                                              "   "         "          "   OMe  Me     N                                 2.971                                                                              "   "         "          "   Me   Me     CH                                2.972                                                                              "   "         "          "   OMe  Cl     CH                                2.973                                                                              "   "         "          Me  Me   OMe    N                                 2.974                                                                              "   "         "          "   OMe  OMe    CH                                2.975                                                                              Me  COCH.sub.2 Br                                                                            CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                2.976                                                                              "   "         "          "   "    "      N                                 2.977                                                                              "   "         "          "   H    Me     N                                 2.978                                                                              "   "         "          "   OMe  Cl     CH                                2.979                                                                              "   "         "          "   Me   Me     CH                                2.980                                                                              "   "         "          "   SMe  NEt.sub.2                                                                             N                                 2.981                                                                              "   "         CO.sub.2 -i-Pr                                                                            Me  OMe  Me     N                                 2.982                                                                              "   "         "          "   OMe  OMe    CH                                2.983                                                                              Me  "         CO.sub.2 -Allyl                                                                           H   OMe  OMe    CH                                2.984                                                                              Et  "         CO.sub.2Me H   OMe  OMe    CH                                2.985                                                                              "   "         "          H   OMe  Me     N                                 2.986                                                                              "   "         "          "   Me   Me     CH                                2.987                                                                              "   "         "          "   Cl   OMe    CH                                2.988                                                                              "   "         "          Me  OMe  OMe    CH                                2.989                                                                              "   "         "          "   OMe  Me     N                                 2.990                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                2.991                                                                              "   "         "          "   OMe  Me     CH                                2.992                                                                              "   "         "          "   Cl   OMe    CH                                2.993                                                                              "   "         "          "   OMe  Me     N                                 2.994                                                                              "   "         "          Me  OMe  OMe    CH                                2.995                                                                              "   "         "          "   "    Me     N                                 2.996                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                2.997                                                                              "   "         "          "   OMe  Me     N                                 2.998                                                                              "   "         "          "   OMe  Cl     CH                                2.999                                                                              "   "         "          "   Me   Me     CH                                3.000                                                                              "   "         "          Me  OMe  OMe    CH                                3.001                                                                              "   "         "          "   OMe  Me     N                                 3.002                                                                              "   "         CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                3.003                                                                              "   "         "          "   OMe  Me     N                                 3.004                                                                              "   "         "          "   Me   Me     CH                                3.005                                                                              "   "         "          Me  OMe  Me     N                                 3.006                                                                              n-Pr                                                                               COCH.sub.2 Br                                                                            CO.sub.2Me H   OMe  OMe    CH                                3.007                                                                              "   "         "          "   "    Cl     CH                                3.008                                                                              "   "         "          "   Me   Me     CH                                3.009                                                                              "   "         "          "   OMe  Me     N                                 3.010                                                                              "   "         "          Me  OMe  OMe    CH                                3.011                                                                              "   "         "          "   OMe  Me     N                                 3.012                                                                              n-Pr                                                                               "         CO.sub.2Et H   "    "      N                                 3.013                                                                              "   "         "          "   "    OMe    CH                                3.014                                                                              "   "         "          "   Me   Me     CH                                3.015                                                                              "   "         CO.sub.2 -n-Pr                                                                            "   OMe  OMe    CH                                3.016                                                                              i-Pr                                                                               "         CO.sub.2Me H   OMe  OMe    CH                                3.017                                                                              "   "         "          "   OMe  Me     N                                 3.018                                                                              "   "         "          "   Me   Me     CH                                3.019                                                                              "   "         "          "   Cl   OMe    N                                 3.020                                                                              "   "         "          Me  OMe  Me     N                                 3.021                                                                              "   "         "          "   "    OMe    CH                                3.022                                                                              Allyl                                                                              "         CO.sub.2Me H   OMe  OMe    CH                                3.023                                                                              "   "         "          "   "    Cl     CH                                3.024                                                                              "   "         "          "   Me   Me     CH                                3.025                                                                              "   "         "          "   OMe  Me     N                                 3.026                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                3.027                                                                              "   "         CO.sub.2 -n-Pr                                                                            "   "    "      CH                                3.028                                                                              "   "         CO.sub.2 -i-Pr                                                                            "   "    "      CH                                3.029                                                                              Me  COCCl.sub.3                                                                              CO.sub.2Me H   OMe  OMe    CH                                3.030                                                                              "   "         "          "   "    OMe    N                                 3.031                                                                              "   "         "          "   "    Me     N                                 3.032                                                                              "   "         "          "   "    "      CH                                3.033                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 3.034                                                                              "   "         "          "   Me   Me     CH                                3.035                                                                              "   "         "          "   "    "      N                                 3.036                                                                              "   "         "          "   Cl   OMe    CH                                3.037                                                                              "   "         "          Me  OMe  OMe    CH                                3.038                                                                              "   "         "          "   "    Me     N                                 3.039                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                3.040                                                                              "   "         "          "   "    Cl     CH                                3.041                                                                              "   "         "          "   Me   Me     CH                                3.042                                                                              "   "         "          "   OMe  Me     N                                 3.043                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 3.044                                                                              "   "         "          Me  OMe  OMe    CH                                3.045                                                                              "   "         "          "   OMe  Me     N                                 3.046                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                3.047                                                                              "   "         "          "   "    "      N                                 3.048                                                                              "   "         "          "   OMe  Me     N                                 3.049                                                                              "   "         "          "   Me   Me     CH                                3.050                                                                              "   "         "          "   OMe  Cl     CH                                3.051                                                                              "   "         "          Me  Me   OMe    N                                 3.052                                                                              "   "         "          "   OMe  OMe    CH                                3.053                                                                              Me  COCCl.sub.3                                                                              CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                3.054                                                                              "   "         "          "   "    "      N                                 3.055                                                                              "   "         "          "   OMe  Me     N                                 3.056                                                                              "   "         "          "   OMe  Cl     CH                                3.057                                                                              "   "         "          "   Me   Me     CH                                3.058                                                                              "   "         "          "   SMe  NEt.sub.2                                                                             N                                 3.059                                                                              "   "         CO.sub.2 -i-Pr                                                                            Me  OMe  Me     N                                 3.060                                                                              "   "         "          "   OMe  OMe    CH                                3.061                                                                              Me  "         CO.sub.2 -Allyl                                                                           H   OMe  OMe    CH                                3.062                                                                              Et  "         CO.sub.2Me H   OMe  OMe    CH                                3.063                                                                              "   "         "          H   OMe  Me     N                                 3.064                                                                              "   "         "          "   Me   Me     CH                                3.065                                                                              "   "         "          "   Cl   OMe    CH                                3.066                                                                              "   "         "          Me  OMe  OMe    CH                                3.067                                                                              "   "         "          "   OMe  Me     N                                 3.068                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                3.069                                                                              "   "         "          "   OMe  Me     CH                                3.070                                                                              "   "         "          "   Cl   OMe    CH                                3.071                                                                              "   "         "          "   OMe  Me     N                                 3.072                                                                              "   "         "          Me  OMe  OMe    CH                                3.073                                                                              "   "         "          "   "    Me     N                                 3.074                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                3.075                                                                              "   "         "          "   OMe  Me     N                                 3.076                                                                              "   "         "          "   OMe  Cl     CH                                3.077                                                                              "   "         "          "   Me   Me     CH                                3.078                                                                              "   "         "          Me  OMe  OMe    CH                                3.079                                                                              "   "         "          "   OMe  Me     N                                 3.080                                                                              "   "         CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                3.081                                                                              "   "         "          "   OMe  Me     N                                 3.082                                                                              "   "         "          "   Me   Me     CH                                3.083                                                                              "   "         "          Me  OMe  Me     N                                 3.084                                                                              n-Pr                                                                               COCCl.sub.3                                                                              CO.sub.2Me H   OMe  OMe    CH                                3.085                                                                              "   "         "          "   "    Cl     CH                                3.086                                                                              "   "         "          "   Me   Me     CH                                3.087                                                                              "   "         "          "   OMe  Me     N                                 3.088                                                                              "   "         "          Me  OMe  OMe    CH                                3.089                                                                              "   "         "          "   OMe  Me     N                                 3.090                                                                              n-Pr                                                                               "         CO.sub.2Et H   "    "      N                                 3.091                                                                              "   "         "          "   "    OMe    CH                                3.092                                                                              "   "         "          "   Me   Me     CH                                3.093                                                                              "   "         CO.sub.2 -n-Pr                                                                            "   OMe  OMe    CH                                3.094                                                                              i-Pr                                                                               "         CO.sub.2Me H   OMe  OMe    CH                                3.095                                                                              "   "         "          "   OMe  Me     N                                 3.096                                                                              "   "         "          "   Me   Me     CH                                3.097                                                                              "   "         "          "   Cl   OMe    N                                 3.098                                                                              "   "         "          Me  OMe  Me     N                                 3.099                                                                              "   "         "          "   "    OMe    CH                                3.100                                                                              Allyl                                                                              "         CO.sub.2Me H   OMe  OMe    CH                                3.101                                                                              "   "         "          "   "    Cl     CH                                3.102                                                                              "   "         "          "   Me   Me     CH                                3.103                                                                              "   "         "          "   OMe  Me     N                                 3.104                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                3.105                                                                              "   "         CO.sub.2 -n-Pr                                                                            "   "    "      CH                                3.106                                                                              "   "         CO.sub.2 -i-Pr                                                                            "   "    "      CH                                3.107                                                                              Me  COCHCl.sub.2                                                                             CO.sub.2Me H   OMe  OMe    CH                                3.108                                                                              "   "         "          "   "    OMe    N                                 3.109                                                                              "   "         "          "   "    Me     N                                 3.110                                                                              "   "         "          "   "    "      CH                                3.111                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 3.112                                                                              "   "         "          "   Me   Me     CH                                3.113                                                                              "   "         "          "   "    "      N                                 3.114                                                                              "   "         "          "   Cl   OMe    CH                                3.115                                                                              "   "         "          Me  OMe  OMe    CH                                3.116                                                                              "   "         "          "   "    Me     N                                 3.117                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                3.118                                                                              "   "         "          "   "    Cl     CH                                3.119                                                                              "   "         "          "   Me   Me     CH                                3.120                                                                              "   "         "          "   OMe  Me     N                                 3.121                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 3.122                                                                              "   "         "          Me  OMe  OMe    CH                                3.123                                                                              "   "         "          "   OMe  Me     N                                 3.124                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                3.125                                                                              "   "         "          "   "    "      N                                 3.126                                                                              "   "         "          "   OMe  Me     N                                 3.127                                                                              "   "         "          "   Me   Me     CH                                3.128                                                                              "   "         "          "   OMe  Cl     CH                                3.129                                                                              "   "         "          Me  Me   OMe    N                                 3.130                                                                              "   "         "          "   OMe  OMe    CH                                3.131                                                                              Me  COCHCl.sub.2                                                                             CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                3.132                                                                              "   "         "          "   "    "      N                                 3.133                                                                              "   "         "          "   OMe  Me     N                                 3.134                                                                              "   "         "          "   OMe  Cl     CH                                3.135                                                                              "   "         "          "   Me   Me     CH                                3.136                                                                              "   "         "          "   SMe  NEt.sub.2                                                                             N                                 3.137                                                                              "   "         CO.sub.2 -i-Pr                                                                            Me  OMe  Me     N                                 3.138                                                                              "   "         "          "   OMe  OMe    CH                                3.139                                                                              Me  "         CO.sub.2 -Allyl                                                                           H   OMe  OMe    CH                                3.140                                                                              Et  "         CO.sub.2Me H   OMe  OMe    CH                                3.141                                                                              "   "         "          H   OMe  Me     N                                 3.142                                                                              "   "         "          "   Me   Me     CH                                3.143                                                                              "   "         "          "   Cl   OMe    CH                                3.144                                                                              "   "         "          Me  OMe  OMe    CH                                3.145                                                                              "   "         "          "   OMe  Me     N                                 3.146                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                3.147                                                                              "   "         "          "   OMe  Me     CH                                3.148                                                                              "   "         "          "   Cl   OMe    CH                                3.149                                                                              "   "         "          "   OMe  Me     N                                 3.150                                                                              "   "         "          Me  OMe  OMe    CH                                3.151                                                                              "   "         "          "   "    Me     N                                 3.152                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                3.153                                                                              "   "         "          "   OMe  Me     N                                 3.154                                                                              "   "         "          "   OMe  Cl     CH                                3.155                                                                              "   "         "          "   Me   Me     CH                                3.156                                                                              "   "         "          Me  OMe  OMe    CH                                3.157                                                                              "   "         "          "   OMe  Me     N                                 3.158                                                                              "   "         CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                3.159                                                                              "   "         "          "   OMe  Me     N                                 3.160                                                                              "   "         "          "   Me   Me     CH                                3.161                                                                              "   "         "          Me  OMe  Me     N                                 3.162                                                                              n-Pr                                                                               COCHCl.sub.2                                                                             CO.sub.2Me H   OMe  OMe    CH                                3.163                                                                              "   "         "          "   "    Cl     CH                                3.164                                                                              "   "         "          "   Me   Me     CH                                3.165                                                                              "   "         "          "   OMe  Me     N                                 3.166                                                                              "   "         "          Me  OMe  OMe    CH                                3.167                                                                              "   "         "          "   OMe  Me     N                                 3.168                                                                              n-Pr                                                                               "         CO.sub.2Et H   "    "      N                                 3.169                                                                              "   "         "          "   "    OMe    CH                                3.170                                                                              "   "         "          "   Me   Me     CH                                3.171                                                                              "   "         CO.sub.2 -n-Pr                                                                            "   OMe  OMe    CH                                3.172                                                                              i-Pr                                                                               "         CO.sub.2Me H   OMe  OMe    CH                                3.173                                                                              "   "         "          "   OMe  Me     N                                 3.174                                                                              "   "         "          "   Me   Me     CH                                3.175                                                                              "   "         "          "   Cl   OMe    N                                 3.176                                                                              "   "         "          Me  OMe  Me     N                                 3.177                                                                              "   "         "          "   "    OMe    CH                                3.178                                                                              Allyl                                                                              "         CO.sub.2Me H   OMe  OMe    CH                                3.179                                                                              "   "         "          "   "    Cl     CH                                3.180                                                                              "   "         "          "   Me   Me     CH                                3.181                                                                              "   "         "          "   OMe  Me     N                                 3.182                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                3.183                                                                              "   "         CO.sub.2 -n-Pr                                                                            "   "    "      CH                                3.184                                                                              "   "         CO.sub.2 -i-Pr                                                                            "   "    "      CH                                3.185                                                                              Me  COCH.sub.2 Cl                                                                            CO.sub.2Me H   OMe  OMe    CH                                3.186                                                                              "   "         "          "   "    OMe    N                                 3.187                                                                              "   "         "          "   "    Me     N                                 3.188                                                                              "   "         "          "   "    "      CH                                3.189                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 3.190                                                                              "   "         "          "   Me   Me     CH                                3.191                                                                              "   "         "          "   "    "      N                                 3.192                                                                              "   "         "          "   Cl   OMe    CH                                3.193                                                                              "   "         "          Me  OMe  OMe    CH                                3.194                                                                              "   "         "          "   "    Me     N                                 3.195                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                3.196                                                                              "   "         "          "   "    Cl     CH                                3.197                                                                              "   "         "          "   Me   Me     CH                                3.198                                                                              "   "         "          "   OMe  Me     N                                 3.199                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 3.200                                                                              "   "         "          Me  OMe  OMe    Ch                                3.201                                                                              "   "         "          "   OMe  Me     N                                 3.202                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                3.203                                                                              "   "         "          "   "    "      N                                 3.204                                                                              "   "         "          "   OMe  Me     N                                 3.205                                                                              "   "         "          "   Me   Me     CH                                3.206                                                                              "   "         "          "   OMe  Cl     CH                                3.207                                                                              "   "         "          Me  Me   OMe    N                                 3.208                                                                              "   "         "          "   OMe  OMe    CH                                3.209                                                                              Me  COCH.sub.2 Cl                                                                            CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                3.210                                                                              "   "         "          "   "    "      N                                 3.211                                                                              "   "         "          "   OMe  Me     N                                 3.212                                                                              "   "         "          "   OMe  Cl     CH                                3.213                                                                              "   "         "          "   Me   Me     CH                                3.214                                                                              "   "         "          "   SMe  NEt.sub.2                                                                             N                                 3.215                                                                              "   "         CO.sub.2 -i-Pr                                                                            Me  OMe  Me     N                                 3.216                                                                              "   "         "          "   OMe  OMe    CH                                3.217                                                                              Me  "         CO.sub.2 -Allyl                                                                           H   OMe  OMe    CH                                3.218                                                                              Et  "         CO.sub.2Me H   OMe  OMe    CH                                3.219                                                                              "   "         "          H   OMe  Me     N                                 3.220                                                                              "   "         "          "   Me   Me     CH                                3.221                                                                              "   "         "          "   Cl   OMe    CH                                3.222                                                                              "   "         "          Me  OMe  OMe    CH                                3.223                                                                              "   "         "          "   OMe  Me     N                                 3.224                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                3.225                                                                              "   "         "          "   OMe  Me     CH                                3.226                                                                              "   "         "          "   Cl   OMe    CH                                3.227                                                                              "   "         "          "   OMe  Me     N                                 3.228                                                                              "   "         "          Me  OMe  OMe    CH                                3.229                                                                              "   "         "          "   "    Me     N                                 3.230                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                3.231                                                                              "   "         "          "   OMe  Me     N                                 3.232                                                                              "   "         "          "   OMe  Cl     CH                                3.233                                                                              "   "         "          "   Me   Me     CH                                3.234                                                                              "   "         "          Me  OMe  OMe    CH                                3.235                                                                              "   "         "          "   OMe  Me     N                                 3.236                                                                              "   "         CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                3.237                                                                              "   "         "          "   OMe  Me     N                                 3.238                                                                              "   "         "          "   Me   Me     CH                                3.239                                                                              "   "         "          Me  OMe  Me     N                                 3.240                                                                              n-Pr                                                                               COCH.sub.2 Cl                                                                            CO.sub.2Me H   OMe  OMe    CH                                3.241                                                                              "   "         "          "   "    Cl     CH                                3.242                                                                              "   "         "          "   Me   Me     CH                                3.243                                                                              "   "         "          "   OMe  Me     N                                 3.244                                                                              "   "         "          Me  OMe  OMe    CH                                3.245                                                                              "   "         "          "   OMe  Me     N                                 3.246                                                                              n-Pr                                                                               "         CO.sub.2Et H   "    "      N                                 3.247                                                                              "   "         "          "   "    OMe    CH                                3.248                                                                              "   "         "          "   Me   Me     CH                                3.249                                                                              "   "         CO.sub.2 -n-Pr                                                                            "   OMe  OMe    CH                                3.250                                                                              i-Pr                                                                               "         CO.sub.2Me H   OMe  OMe    CH                                3.251                                                                              "   "         "          "   OMe  Me     N                                 3.252                                                                              "   "         "          "   Me   Me     CH                                3.253                                                                              "   "         "          "   Cl   OMe    N                                 3.254                                                                              "   "         "          Me  OMe  Me     N                                 3.255                                                                              "   "         "          "   "    OMe    CH                                3.256                                                                              Allyl                                                                              "         CO.sub.2Me H   OMe  OMe    CH                                3.257                                                                              "   "         "          "   "    Cl     CH                                3.258                                                                              "   "         "          "   Me   Me     CH                                3.259                                                                              "   "         "          "   OMe  Me     N                                 3.260                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                3.261                                                                              "   "         CO.sub.2 -n-Pr                                                                            "   "    "      CH                                3.262                                                                              "   "         CO.sub.2 -i-Pr                                                                            "   "    "      CH                                3.263                                                                              Me  COCF.sub.3                                                                               CO.sub.2 Me                                                                               H   OMe  OMe    CH                                3.264                                                                              "   "         "          "   "    OMe    N                                 3.265                                                                              "   "         "          "   "    Me     N                                 3.266                                                                              "   "         "          "   "    "      CH                                3.267                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 3.268                                                                              "   "         "          "   Me   Me     CH                                3.269                                                                              "   "         "          "   "    "      N                                 3.270                                                                              "   "         "          "   Cl   OMe    CH                                3.271                                                                              "   "         "          Me  OMe  OMe    CH                                3.272                                                                              "   "         "          "   "    Me     N                                 3.273                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                3.274                                                                              "   "         "          "   "    Cl     CH                                3.275                                                                              "   "         "          "   Me   Me     CH                                3.276                                                                              "   "         "          "   OMe  Me     N                                 3.277                                                                              "   "         "          "   NMe.sub.2                                                                           OCH.sub.2 CF.sub.3                                                                    N                                 3.278                                                                              "   "         "          Me  OMe  OMe    CH                                3.279                                                                              "   "         "          "   OMe  Me     N                                 3.280                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                3.281                                                                              "   "         "          "   "    "      N                                 3.282                                                                              "   "         "          "   OMe  Me     N                                 3.283                                                                              "   "         "          "   Me   Me     CH                                3.284                                                                              "   "         "          "   OMe  Cl     CH                                3.285                                                                              "   "         "          Me  Me   OMe    N                                 3.286                                                                              "   "         "          "   OMe  OMe    CH                                3.287                                                                              Me  COCF.sub.3                                                                               CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                3.288                                                                              "   "         "          "   "    "      N                                 3.289                                                                              "   "         "          "   OMe  Me     N                                 3.290                                                                              "   "         "          "   OMe  Cl     CH                                3.291                                                                              "   "         "          "   Me   Me     CH                                3.292                                                                              "   "         "          "   SMe  NEt.sub.2                                                                             N                                 3.293                                                                              "   "         CO.sub.2 -i-Pr                                                                            Me  OMe  Me     N                                 3.294                                                                              "   "         "          "   OMe  OMe    CH                                3.295                                                                              Me  "         CO.sub.2 -Allyl                                                                           H   OMe  OMe    CH                                3.296                                                                              Et  "         CO.sub.2Me H   OMe  OMe    CH                                3.297                                                                              "   "         "          H   OMe  Me     N                                 3.298                                                                              "   "         "          "   Me   Me     CH                                3.299                                                                              "   "         "          "   Cl   OMe    CH                                3.300                                                                              "   "         "          Me  OMe  OMe    CH                                3.301                                                                              "   "         "          "   OMe  Me     N                                 3.302                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                3.303                                                                              "   "         "          "   OMe  Me     CH                                3.304                                                                              "   "         "          "   Cl   OMe    CH                                3.305                                                                              "   "         "          "   OMe  Me     N                                 3.306                                                                              "   "         "          Me  OMe  OMe    CH                                3.307                                                                              "   "         "          "   "    Me     N                                 3.308                                                                              "   "         CO.sub.2 -n-Pr                                                                            H   OMe  OMe    CH                                3.309                                                                              "   "         "          "   OMe  Me     N                                 3.310                                                                              "   "         "          "   OMe  Cl     CH                                3.311                                                                              "   "         "          "   Me   Me     CH                                3.312                                                                              "   "         "          Me  OMe  OMe    CH                                3.313                                                                              "   "         "          "   OMe  Me     N                                 3.314                                                                              "   "         CO.sub.2 -i-Pr                                                                            H   OMe  OMe    CH                                3.315                                                                              "   "         "          "   OMe  Me     N                                 3.316                                                                              "   "         "          "   Me   Me     CH                                3.317                                                                              "   "         "          Me  OMe  Me     N                                 3.318                                                                              n-Pr                                                                               COCF.sub.3                                                                               CO.sub.2Me H   OMe  OMe    CH                                3.319                                                                              "   "         "          "   "    Cl     CH                                3.320                                                                              "   "         "          "   Me   Me     CH                                3.321                                                                              "   "         "          "   OMe  Me     N                                 3.322                                                                              "   "         "          Me  OMe  OMe    CH                                3.323                                                                              "   "         "          "   OMe  Me     N                                 3.324                                                                              n-Pr                                                                               "         CO.sub.2Et H   "    "      N                                 3.325                                                                              "   "         "          "   "    OMe    CH                                3.326                                                                              "   "         "          "   Me   Me     CH                                3.327                                                                              "   "         CO.sub.2 -n-Pr                                                                            "   OMe  OMe    CH                                3.328                                                                              i-Pr                                                                               "         CO.sub.2Me H   OMe  OMe    CH                                3.329                                                                              "   "         "          "   OMe  Me     N                                 3.330                                                                              "   "         "          "   Me   Me     CH                                3.331                                                                              "   "         "          "   Cl   OMe    N                                 3.332                                                                              "   "         "          Me  OMe  Me     N                                 3.333                                                                              "   "         "          "   "    OMe    CH                                3.334                                                                              Allyl                                                                              "         CO.sub.2Me H   OMe  OMe    CH                                3.335                                                                              "   "         "          "   "    Cl     CH                                3.336                                                                              "   "         "          "   Me   Me     CH                                3.337                                                                              "   "         "          "   OMe  Me     N                                 3.338                                                                              "   "         CO.sub.2Et H   OMe  OMe    CH                                3.339                                                                              "   "         n-Pr       "   "    "      CH                                3.340                                                                              "   "         i-Pr       "   "    "      CH                                3.341                                                                              Me  COCH.sub.3                                                                               CHO        "   "    "      CH                                3.342                                                                              "   CO.sub.2 CH.sub.3                                                                        "          "   "    "      CH                                3.343                                                                              "   COCH.sub.3                                                                               COCH.sub.3 "   "    "      CH                                3.344                                                                              "   CO.sub.2 CH.sub.3                                                                        "          "   "    "      CH                                3.345                                                                              "   COCH.sub.3                                                                               COS-i-Pr   "   "    "      CH                                3.346                                                                              "   CO.sub.2 Et                                                                              "          "   "    "      CH                                3.347                                                                              "   CHO       CONMe.sub.2                                                                               "   "    "      CH                                3.348                                                                              "   "         "          "   OMe  Me     N                                 3.349                                                                              "   COCH.sub.3                                                                               "          "   OMe  OMe    CH                                3.350                                                                              "   "         CONH.sub.2 "   "    "      CH                                3.351                                                                              "   COCH.sub.3                                                                               CSNMe.sub.2                                                                               "   OMe  OMe    CH                                3.352                                                                              "   CO.sub.2 Et                                                                              "          "   "    "      CH                                3.353                                                                              "   COCH.sub.2 CH.sub.3                                                                      "          "   "    "      CH                                3.354                                                                              "   CO.sub.2 Me                                                                              CSO-i-Pr   "   "    "      CH                                3.355                                                                              "   CHO       "          "   "    "      CH                                3.356                                                                              "   "         C(NNMe.sub.2)H                                                                            "   "    "      CH                                3.357                                                                              Me  COCH.sub.3                                                                               C(NOMe)OMe H   OMe  OMe    CH                                3.358                                                                              "   CO.sub.2 CH.sub.3                                                                        H          "   "    "      CH                                3.359                                                                              "   CHO       "          "   "    "      CH                                3.360                                                                              "   "         C(NOH)H    "   "    "      CH                                3.361                                                                              "   CO.sub.2 Me                                                                              "          "   "    "      CH                                3.362                                                                              "   COCH.sub.3                                                                               C(NOMe)H   "   "    "      CH                                3.363                                                                              "   "         CO.sub.2 H "   "    "      CH                                3.364                                                                              "   CO.sub.2 Me                                                                              "          "   "    "      CH                                3.365                                                                              "   COCH.sub.3                                                                               C(NEt)OMe  "   "    "      CH                                3.366                                                                              "   "         C(N-i-Pr)H "   "    "      CH                                3.367                                                                              "   CO.sub.2 CH.sub.2 CH.sub.2 Cl                                                            COOMe      H   OMe  OMe    CH  141-143                       3.368                                                                              "   "         "          H   "    "      CH  123-126                       __________________________________________________________________________ 

We claim:
 1. A compound of the formula (II) ##STR31## wherein R¹ is C₁ -C₆ -alkyl, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, the 3 latter radicals independently of one another being unsubstituted or substituted by one or more radicals from the group consisting of halogen, C₁ -C₄ -alkoxy, CONH₂, C₁ -C₄ -alkylthio, CN, CHO, (C₁ -C₆ -alkyl)carbonyl, (C₃ -C₆ -cycloalkyl)carbonyl, C₁ -C₄ alkylsulfonyl, carboxyl, (C₁ -C₄ -alkoxy)carbonyl, (C₂ -C₄ -alkenyloxy)carbonyl, (C₂ -C₄ -alkynyloxy)carbonyl, NO₂, NH₂, mono- and di-(C₁ -C₆)-alkylamino,R² is CO--R⁵, COO--R⁶, CO--SR⁷, CO--NR⁸ R⁹, CS--NR¹⁰ R¹¹, CS--OR¹², CS--SR¹³, SO₂ R¹⁴, SO₂ NR¹⁵ R¹⁶, R³ is COR¹⁷, CO--OR¹⁸, CO--NR¹⁹ R²⁰, CO--SR²¹, COO--N═CR²² R²³, CSR²⁴, CSSR²⁵, CS--OR²⁶, CS--NR²⁷ R²⁸, C(═NR²⁹)R³⁰, R⁵ is H, C₁ -C₆ -alkyl, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, the three latter radicals independently of one another being unsubstituted or substituted by one or more radicals from the group, consisting of halogen, C₁ -C₄ -alkoxy, C₁ -C₄ -alkylthio and NR³¹ R³², or unsubstituted or substituted C₃ -C₈ -cycloalkyl, unsubstituted or substituted phenyl, unsubstituted or substituted heteroaryl or phenyl-C₁ -C₄ -alkyl which is unsubstituted or substituted on the phenyl ring, R⁶ is C₁ -C₆ -alkyl, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, the three latter radicals independently of one another being unsubstituted or substituted by one or more radicals from the group consisting of halogen, C₁ -C₄ -alkoxy, C₁ -C₄ -alkylthio and NR³¹ R³², or C₃ -C₆ -cycloalkyl which is unsubstituted or substituted by one or more radicals from the group consisting of halogen, C₁ -C₄ -alkyl and C₁ -C₄ -alkoxy, or C₃ -C₆ -cycloalkyl-C₁ -C₃ -alkyl, R⁷ is as defined in R⁶ R⁸ is H, C₁ -C₆ -alkyl, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, the 3 latter radicals independently of one another being unsubstituted or substituted by one or more radicals from the group consisting of halogen, or (C₁ -C₆)-alkoxy)carbonyl or C₁ -C₄ -alkoxy, R⁹ is H, C₁ -C₆ -alkyl, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, the 3 latter radicals independently of one another being unsubstituted or substituted by one or more radicals from the group consisting of halogen, C₁ -C₄ -alkoxy, C₁ -C₄ -alkylthio and NR³¹ R³², or CO--R³³, CO--OR³⁴, CO--NR³⁵ R³⁶, CS--NR³⁵ R³⁶, CS--R³³ or CS--OR³⁴, or R⁸, R⁹ taken together are a divalent radical of the formula --(CH₂)₄ --, --(CH₂)₅ --, --CH₂ CH₂ --O--CH₂ CH₂ --CH₂ CH₂ NHCH₂ CH₂ --, the 4 latter radicals being unsubstituted or substituted by C₁ -C₄ -alkyl, R¹⁰ is as defined in R⁸, R¹¹ is as defined in R⁹, R¹² is as defined in R⁶, R¹³ is as defined in R⁶, R¹⁴ is C₁ -C₆ -alkyl, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, the three latter radicals independently of one another being unsubstituted or substituted by one or more radicals from the group consisting of halogen, C₁ -C₄ -alkoxy, C₁ -C₄ -alkylthio and NR³¹ R³², R¹⁵ is as defined in R⁸, R¹⁶ is H, C₁ -C₆ -alkyl, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, the 3 latter radicals independently of one another being unsubstituted or substituted by one or more halogen radicals, R¹⁷ is as defined in R⁵, R¹⁸ is C₁ -C₆ -alkyl, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, the three latter radicals independently of one another being unsubstituted or substituted by one or more radicals from the group consisting of halogen, C₁ -C₄ -alkoxy, C₁ -C₄ -alkylthio and NR³¹ R³², or C₃ -C₆ -cycloalkyl which is unsubstituted or substituted by one or more radicals from the group consisting of halogen, C₁ -C₄ -alkyl and C₁ -C₄ -alkoxy, or C₃ -C₆ -cycloalkyl-C₁ -C₃ -alkyl or H, R¹⁹ is as defined in R⁸, R²⁰ is as defined in R⁹, R²¹ is as defined in R¹⁸, R²² is H, C₁ -C₄ -alkyl, C₃ -C₅ -alkenyl or C₃ -C₅ -alkynyl, R²³ is H, C₁ -C₄ -alkyl, C₃ -C₅ -alkenyl or C₃ -C₅ -alkynyl, R²⁴ is as defined in R¹⁷, R²⁵ is as defined in R¹⁸, R²⁶ is as defined in R¹⁸, R²⁷ is as defined in R⁸, R²⁸ is as defined in R⁹, R²⁹ is H, OH, NH₂, NHR³⁷, N(R³⁷)₂, C₁ -C₄ -alkyl, C₁ -C₄ -alkoxy, C₂ -C₄ -alkenyl or C₂ -C₄ -alkynyl, the 4 latter radicals independently of one another being unsubstituted or substituted by one or more radicals from the group consisting of halogen, C₁ -C₃ -alkoxy and C₁ -C₃ -alkylthio, R³⁰ is H, C₁ -C₆ -alkyl, C₁ -C₆ -alkoxy, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, the four latter radicals independently of one another being unsubstituted or substituted by one or more radicals from the group consisting of halogen, C₁ -C₃ -alkoxy and C₁ -C₃ -alkylthio, each R³¹ independently of the others is H, C₁ -C₄ -alkyl, (C₁ -C₄ -alkyl)carbonyl, (C₁ -C₄ -alkoxy)carbonyl or CHO, each R³² independently of the others is H or C₁ -C₄ -alkyl, R³³ is as defined in R⁵, R³⁴ is as defined in R⁶, R³⁵, R³⁶ independently of one another are H, C₁ -C₆ -alkyl, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, the 3 latter radicals independently of one another being unsubstituted or substituted by one or more halogen radicals, R³⁷ is C₁ -C₄ -alkyl, C₂ -C₄ -alkenyl or C₂ -C₄ -alkynyl, the three radicals mentioned, independently of one another, being unsubstituted or substituted by one or more radicals from the group consisting of halogen, C₁ -C₄ -alkoxy and C₁ -C₄ -alkylthio.
 2. A compound as claimed in claim 1 whereinR¹ is C₁ -C₄ -alkyl, C₂ -C₄ -alkenyl or C₂ -C₄ -alkynyl, or R² is CO--R⁵, COOR⁶, CO--NR⁸ R⁹, CS--NR¹⁰ R¹¹, SO₂ R¹⁴ or SO₂ NR¹⁵ R¹⁶, or R³ is COR¹⁷, COOR¹⁸, CONR¹⁹ R²⁰ or CO--ON═CR²² R²³, or R⁵ is H, C₁ -C₆ -alkyl which is unsubstituted or substituted by one or more halogen atoms, or by C₁ -C₄ -alkoxy, C₁ -C₄ -alkylthio or NR³¹ R³², or is C₃ -C₆ -cycloalkyl, phenyl, benzyl or heteroaryl, the three latter radicals being unsubstituted or substituted by one or more radicals from the group consisting of C₁ -C₄ -alkyl, C₁ -C₄ -alkoxy and halogen, or R⁶ is C₁ -C₆ -alkyl, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, C₁ -C₆ -haloalkyl or C₃ -C₆ -cycloalkyl, or R⁷ is C₁ -C₄ -alkyl, R⁸ is hydrogen, C₁ -C₆ -alkyl, C₁ -C₄ -haloalkyl, C₁ -C₄ -alkoxy or (C₁ -C₄ -alkoxy)carbonyl, R⁹ is hydrogen, C₁ -C₆ -alkyl which is unsubstituted or substituted by one or more radicals from the group consisting of halogen, C₁ -C₄ -alkoxy and NR³¹ R³², or CO--R³³, CO--OR³⁴ or CO--NR³⁵ R³⁶, or R⁸ and R⁹ taken together are a divalent radical of the formula --(CH₂)₄ --, --(CH₂)₅ -- or --CH₂ CH₂ --O--CH₂ CH₂ --, or R¹⁴ is C₁ -C₆ -alkyl or C₁ -C₆ -haloalkyl, or R¹⁵, R¹⁶ independently of one another are hydrogen or C₁ -C₄ -alkyl, or R¹⁷ is hydrogen or C₁ -C₄ -alkyl, C₁ -C₄ -haloalkyl, C₃ -C₆ -cycloalkyl, phenyl or heteroaryl, the two latter radicals being unsubstituted or substituted, or R¹⁸ is hydrogen, C₁ -C₄ -alkyl, C₂ -C₆ -alkenyl or C₂ -C₆ -alkynyl, the 3 latter radicals being unsubstituted or substituted by one or more radicals from the group consisting of halogen, C₁ -C₄ -alkoxy, C₁ -C₄ -alkylthio and NR³¹ R³², or C₃ -C₆ -cycloalkyl or C₃ -C₆ -cycloalkyl-C₁ -C₃ -alkyl, or R²² is hydrogen or C₁ -C₂ -alkyl, or R²³ is hydrogen or C₁ -C₂ -alkyl, or R²⁹ is hydrogen, hydroxyl, amino, NHCH₃, N(CH₃)₂, C₁ -C₄ -alkyl or C₁ -C₄ -alkoxy, R³⁰ is hydrogen or C₁ -C₄ -alkyl, or each R³¹ independently of the others is H or C₁ -C₄ -alkyl, or each R³² independently of the others is H or C₁ -C₄ -alkyl, or R³³ is hydrogen, C₁ -C₄ -alkyl, C₁ -C₄ -haloalkyl, C₃ -C₆ -cycloalkyl or phenyl which is unsubstituted or substituted by one or more radicals from the group consisting of halogen, C₁ -C₄ -alkyl and C₁ -C₄ -alkoxy, or R³⁴ is C₁ -C₄ -alkyl, allyl, propargyl or cycloalkyl, or R³⁵ is hydrogen or C₁ -C₄ -alkyl, or R³⁶ is hydrogen or C₁ -C₄ -alkyl.
 3. A compound as claimed in claim 1 whereinR¹ is methyl, ethyl, n-propyl, i-propyl or allyl, R² is CO--R⁵, COOR⁶, CO--NR⁸ R⁹, CS--NR¹⁰ R¹¹, SO₂ R¹⁴ or SO₂ NR¹⁵ R¹⁶, R⁵ is H, C₁ -C₄ -alkyl, C₁ -C₂ -haloalkyl, cyclopropyl, phenyl, benzyl or heteroaryl having 5 or 6 ring atoms, the 3 latter radicals being unsubstituted or substituted by one or more halogen atoms, R⁶ is C₁ -C₄ -alkyl, allyl, propargyl or cyclopropyl, R⁸ is H, C₁ -C₄ -alkyl, C₁ -C₄ -haloalkyl or (C₁ -C₄ -alkoxy)carbonyl, R⁹ is H or C₁ -C₄ -alkyl, R¹⁰ is H or C₁ -C₄ -alkyl, R¹¹ is H or C₁ -C₄ -alkyl, R¹⁴ is C₁ -C₄ -alkyl, R¹⁵ is H or C₁ -C₄ -alkyl and R¹⁶ is H or C₁ -C₄ -alkyl.
 4. A compound as claimed in claim 1, whereinR⁵ is H, CH₃, C₂ H₅, n- or i-C₃ H₇, n-, i-, t- or 2-butyl, n-pentyl, CF₃, CH₂ Cl, CHCl₂, CCl₃, CH₂ Br, CH₂ CCl₃, cyclopropyl, phenyl, thienyl, furyl or pyridyl, in which case the 4 latter radicals may be substituted by from 1 to 3 halogen atoms.
 5. A compound as claimed in claim 3, whereinR⁵ is H, CH₃, C₂ H₅, n- or i-C₃ H₇, n-, i-, t- or 2-butyl, n-pentyl, CF₃, CH₂ Cl, CHCl₂, CCl₃, CH₂ Br, CH₂ CCl₃, cyclopropyl, phenyl, thienyl, furyl or pyridyl, in which case the 4 latter radicals may be substituted by from 1 to 3 halogen atoms.
 6. A compound as claimed in claim 1, whereinR¹ is methyl, ethyl, n-propyl, i-propyl or allyl, R² is formyl, acetyl, methoxycarbonyl, ethoxycarbonyl, 2-chloroethoxycarbonyl, ethoxycarbonylaminothiocarbonyl, methylaminosulfonyl, methylsulfonyl, and R³ is methoxycarbonyl or ethoxycarbonyl.
 7. A compound as claimed in claim 1, whereinR¹ is methyl, ethyl, n-propyl, i-propyl or allyl, R² is formyl, acetyl, methoxycarbonyl, ethoxycarbonyl, and R³ is methoxycarbonyl. 